Heterocyclic Building Blocks-Tetrahydroisoquinoline

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 882562-40-5, is researched, Molecular C18H11Cl2N3O2S, about Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors, the main research direction is THZ531 CDK12 CDK13 inhibitor transcription cancer.Formula: C18H11Cl2N3O2S.

Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription. However, the absence of CDK12 and CDK13 inhibitors has hindered the ability to investigate the consequences of their inhibition in healthy cells and cancer cells. Here we describe the rational design of a first-in-class CDK12 and CDK13 covalent inhibitor, THZ531. Co-crystallization of THZ531 with CDK12-cyclin K indicates that THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. In particular, THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes. Coincident with transcriptional perturbation, THZ531 dramatically induced apoptotic cell death. Small mols. capable of specifically targeting CDK12 and CDK13 may thus help identify cancer subtypes that are particularly dependent on their kinase activities.

Compound(882562-40-5)Formula: C18H11Cl2N3O2S received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole), if you are interested, you can check out my other related articles.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Picolinamide(SMILESS: O=C(N)C1=NC=CC=C1,cas:1452-77-3) is researched.COA of Formula: C8H11NO2. The article 《Screening a trace amount of pharmaceutical cocrystals by using an enhanced nano-spot method》 in relation to this compound, is published in European Journal of Pharmaceutics and Biopharmaceutics. Let’s take a look at the latest research on this compound (cas:1452-77-3).

Cocrystn. is an attractive and promising technol. that can improve the phys. properties of formulations of active pharmaceutical ingredients (APIs). We have developed a “”nano-spot method”” that can evaluate the crystalline form on the nanogram scale. In this study, the following studies were performed to obtain versatile and comprehensive improvements to the nano-spot method: modification of the sample solution, application of solvent vapor exposure to attempt the precipitation of various states of crystals, and adoption of low-frequency Raman spectroscopy. Carbamazepine was used as a model API and cocrystn. screening was examined with 12 cocrystal formers (coformers). In the case of combinations that are already known to form cocrystals, spectra similar to those of previously reported cocrystals or new spectra were obtained. It was considered that the reported cocrystals or new polymorphs were obtained. In contrast, in the case of the combination which has been reported not to form a cocrystal, the spectra were consistent with that for the phys. mixture of API and coformer, suggesting that a cocrystal also did not form in this screening. In addition, the newly adopted low-frequency Raman spectroscopy enabled the high-sensitive detection of the crystalline form.

Compound(1452-77-3)Reference of Picolinamide received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(Picolinamide), if you are interested, you can check out my other related articles.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ) is researched.Name: cis-Dichlorobis(pyridine)platinum(II).Lasitsa, N. A.; Skvortsov, N. K.; Lobadyuk, V. I.; Spevak, V. N.; Esina, G. A.; Abramova, I. P.; Lazarev, S. Ya. published the article 《Platinum(II) complexes in the catalytic hydrosilylation of acetophenone. Kinetics of the reaction and the effect of ligands》 about this compound( cas:15227-42-6 ) in Zhurnal Obshchei Khimii. Keywords: acetophenone hydrosilylation platinum catalyst kinetics; ligand effect platinum catalyst hydrosilylation. Let’s learn more about this compound (cas:15227-42-6).

A kinetic study of hydrosilylation of MeCOPh with MeSiHCl2 or MeSiPhH2 in the presence of LL1PtX2 (X = Cl, Br; L = L1 = Me2SO, Et2SO, py, Et3P, MeSOC6H4Me-4; L = C2H4, L1 = Me2SO, Et2SO; L = py, L1 = Et2SO; L = MeSOC6H4Me-4, L1 = Bu3P) catalysts showed a relationship between the ligand type and catalytic activity. In contrast with bis(phosphine) and bis(olefin) complexes, bis(sulfoxide) complexes and all complexes with mixed ligands, one of which is sulfoxide, show high catalytic activity. For the reaction with MeSiHCl2, the order of reactivity is olefin > SO > P(III) > py, close to an analogous relationship for the hydrosilylation of olefins.

Compound(15227-42-6)Name: cis-Dichlorobis(pyridine)platinum(II) received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(cis-Dichlorobis(pyridine)platinum(II)), if you are interested, you can check out my other related articles.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

HPLC of Formula: 15227-42-6. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Synthesis of potential platinum(II) antitumor complexes: complexes containing bidentate pyridyl and imidazolyl donors.

PtLCl2 [L = di-2-pyridylmethane, 3,3-bis(2-pyridyl)pentane, 2-(2-pyridyl)imidazole (I), N-methyl-2-(2-pyridyl)imidazole] were prepared and characterized by chem. anal., elec. conductivity, IR spectra, and inhibitory effects on cultures of L1210 mouse leukemia cells. The complex with L = I gave a 50% inhibiting dose similar to that of cis-Pt(NH3)2Cl2 and below the values of the other complexes; this suggests that further tests with tumor-bearing animals is warranted for this I complex with Pt.

Compound(15227-42-6)HPLC of Formula: 15227-42-6 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(cis-Dichlorobis(pyridine)platinum(II)), if you are interested, you can check out my other related articles.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Application of 1452-77-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Highly Efficient Synthesis of Alkyl N-Arylcarbamates from CO2, Anilines, and Branched Alcohols with a Catalyst System of CeO2 and 2-Cyanopyridine. Author is Gu, Yu; Miura, Ayaka; Tamura, Masazumi; Nakagawa, Yoshinao; Tomishige, Keiichi.

Highly efficient synthesis of alkyl N-arylcarbamates from CO2, anilines, and alcs. using the CeO2 and 2-cyanopyridine catalyst system was substantiated by selecting branched alcs., such as 2-propanol and cyclohexanol, with minimized formation of byproducts, such as dialkyl carbonates and picolinamide. The catalyst system is operable even at low CO2 pressure (≤1 MPa), and the target carbamates were obtained with high arylamine-based yields (up to 94%). Alkyl N-phenylcarbamates were obtained from CO2, anilines, and alcs. with high yield and minimized formation of byproducts by using branched alcs.

Compound(1452-77-3)Application of 1452-77-3 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(Picolinamide), if you are interested, you can check out my other related articles.

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Adducts of coordination compounds – 12. New hydrogen dinitrates and their structures》. Authors are Al-Zamil, Nabila S.; Evans, E. H. M.; Gillard, R. D.; James, David W.; Jenkins, Tudor E.; Lancashire, Robert J.; Williams, P. A..The article about the compound:cis-Dichlorobis(pyridine)platinum(II)cas:15227-42-6,SMILESS:[Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2).Category: tetrahydroisoquinoline. Through the article, more information about this compound (cas:15227-42-6) is conveyed.

The new compounds trans-[Ru(py)4Cl2][H(ONO2)2] and [C13H9NH][H(ONO2)2] were characterized (C13H9N = phenanthridine) and these, with the known compounds trans-[Ir(py)4Cl2][H(ONO2)2], C13H9N.2HNO3.2H2O and [phenH][H(ONO2)2] (phen = 1,10-phenanthroline) shown to involve the H dinitrate ion. The crystal and mol. structure of the Ru complex was determined The orthorhombic unit cell, space group Pbcn has a 7.54, b 21.83, c 14.86 (±0.01) Å, Z = 4. The compound is isomorphous with the analogous Rh(III) complex, but has addnl. disorder involving the nitrate groups owing to loss of HNO3 with time to yield an isostructural mononitrate compound trans-[Ru(py)4Cl2][H(ONO2)2] and trans-[Pt(py)4Cl2](NO3)2 were obtained under conditions previously described as giving rise to nitration of the pyridine ring. In fact, no evidence for the formation of 3-nitropyridine was found during these studies.

If you want to learn more about this compound(cis-Dichlorobis(pyridine)platinum(II))Category: tetrahydroisoquinoline, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(15227-42-6).

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

HPLC of Formula: 15227-42-6. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Thermal migration of amines in platinum(II) complexes. Author is Kukushkin, Yu. N.; Sedova, G. N.; Belyaev, A. N..

Derivatog. data indicate that the 1st stage of the thermal conversion of (LH)2[PtCl4] (L = NH3, MeNH2, piperidine, pyridine, γ-picoline, PhNH2, p-toluidine, 8-hydroxyquinoline, quinoline) or (enH2)[PtCl4] is the cleavage of HCl and the formation of PtL2Cl2. All the complexes studied fall into 2 groups according to the temperature of the beginning of the process: (1) complexes with a temperature for the start of thermal reaction at 180 – 200° contain amines the basicity constants of which are >10-5 and (2) complexes with decomposition temperatures at 130-50° contain amines the basicity constants of which are <10-8. If you want to learn more about this compound(cis-Dichlorobis(pyridine)platinum(II))HPLC of Formula: 15227-42-6, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(15227-42-6).

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Synthesis and evaluation of 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide for PET imaging of the metabotropic glutamate receptor 2 in the rat brain, the main research direction is carbon 11 fluoromethoxyphenyl methylpyridinyl methoxypicolinamide preparation brain mGluR2 PET; In vitro autoradiography; Metabotropic glutamate receptor 2; Positron emission tomography; Radiotracer; Schizophrenia.Related Products of 1452-77-3.

Metabotropic glutamate receptor 2 (mGluR2) has been suggested as a therapeutic target for treating schizophrenia-like symptoms arising from increased glutamate transmission in the human forebrain. However, no reliable positron emission tomog. (PET) radiotracer allowing for in vivo visualization of mGluR2 in the human brain is currently available. In this study, we synthesized 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide ([11C]1) and evaluated its potential as a PET tracer for imaging mGluR2 in the rodent brain. Compound 1, a neg. allosteric modulator (NAM) of mGluR2, showed high in vitro binding affinity (IC50: 26 nM) for mGluR2 overexpressed in human cells. [11C]1 was synthesized by O-[11C]methylation of the phenol precursor 2 with [11C]methyl iodide. After the reaction, HPLC purification and formulation, [11C]1 of 7.4 ± 2.8 GBq (n = 8) was obtained from [11C]carbon dioxide of 22.5 ± 4.8 GBq (n = 8) with >99% radiochem. purity and 70 ± 32 GBq/μmol (n = 8) molar activity at the end of synthesis. In vitro autoradiog. for rat brains showed that [11C]1 binding was heterogeneously distributed in the cerebral cortex, striatum, hippocampus, and cerebellum. This pattern is consistent with the regional distribution pattern of mGluR2 in the rodent brain. The radioactivity was significantly reduced by self- or MNI-137 (a mGluR2 NAM) blocking. Small-animal PET studies indicated a low in vivo specific binding of [11C]1 in the rat brain. The brain uptake was increased in a P-glycoprotein and breast cancer resistant protein double knockout mouse, when compared to a wild-type mouse. While [11C]1 presented limited potential as an in vivo PET tracer for mGluR2, we suggested that it can be used as a lead compound for developing new radiotracers with improved in vivo brain properties.

If you want to learn more about this compound(Picolinamide)Related Products of 1452-77-3, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(1452-77-3).

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 15227-42-6, is researched, Molecular C10H10Cl2N2Pt, about Activation of the trans geometry in platinum antitumor complexes: a survey of the cytotoxicity of trans complexes containing planar ligands in murine L1210 and human tumor panels and studies on their mechanism of action, the main research direction is trans platinum antitumor complex resistance structure.Recommanded Product: cis-Dichlorobis(pyridine)platinum(II).

The cytotoxicity of transplatinum complexes of structural formula trans-[PtCl2(L)L’)] {L = L’ = pyridine or thiazole, or L = quinoline (R’ = methyl; R” = Me, Ph or CH2phenyl) and L’ = R’R”SO] has been studied in murine L1210 and human tumor cell lines. The results confirm previous observations that use of a sterically hindered planar ligand greatly enhances cytotoxicity, in comparison to trans-[PtCl2(NH3)2], such that in some cases cytotoxicity equivalent to that of the clin. used agent cisplatin [cis-{PtCl2(NH3)2]] is obtained. Results from both the panel of human ovarian carcinoma cell lines and the National Cancer Institute screening panel confirm a different pattern of cytotoxicity, with respect to cisplatin. The new trans-platinum complexes are also non-cross-resistant with cisplatin in both murine and human (human ovarian carcinoma panel) tumor cell lines. Preliminary mechanistic studies using both cis- and trans-[PtCl2(pyridine)2] in L1210 cells have been carried out, to delineate the reasons for both the dramatically enhanced cytotoxicity and the lack of cross-resistance with the clin. used agents. Intracellular uptake is enhanced for pyridine relative to ammine (NH3) complexes. The pyridine complexes also inhibit DNA synthesis, implying a role for DNA binding in their mechanism of action. Binding of the pyridine complexes to calf thymus DNA is, however, significantly less than for the analogous ammine complexes. The presence of trans-pyridine ligands results in steric hindrance, which retards the rate of reaction of trans-[PtCl2(pyridine)2], relative to trans[PtCl2(NH3)2], with other important biomols. such as glutathione. The results point to a potential new class of platinum antitumor complexes acting by a new mechanism and with activity complementary to agents such as cisplatin.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Recommanded Product: 693-67-4. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Multiresponse Shape-Memory Nanocomposite with a Reversible Cycle for Powerful Artificial Muscles.

In the field of bionic soft robots and microrobots, artificial muscle materials have exhibited unique potential for cutting-edge applications. However, current mainstream thermal-responsive artificial muscles based on semicrystalline polymers (SCPs), despite their excellent phys. properties, suffer from the limitation of environmental stimuli in practice, while their photodriven counterparts adopting liquid crystal elastomers (LCEs) lack ductility. Herein, a novel multifunctional programmable artificial muscle with a unique patch-sewing structure formed by π-π stacking between azobenzene groups was designed, which combined the advantages of SCPs and LCEs. The nanocomposite demonstrated a unique combination between artificial muscle performance (46.5 times the energy d. and 26.6 times the power d. of human skeletal muscles) and programmability (274.84% strain and 100% shape-memory recovery rate within 1 s). Meanwhile, coupling the photoisomerization of azobenzene and the photothermal conversion of gold nanorods, the cycle of deformation triggered by UV light and restoring by IR light could be accomplished rapidly within 30 s. A COMSOL Multiphysics model was established and the corresponding finite element anal. verified the photoactuation and captured the general principle of light initiation in elastomers. These demonstrate that the multifunctional programmable elastomer is promising for artificial muscle applications, especially for photoinduced actuation.

If you want to learn more about this compound(1-Bromoundecane)Recommanded Product: 693-67-4, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(693-67-4).

Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem