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The invention discloses an optical pure 2 – tetrahydrofurfuryl acid preparation process, it will L – phenylalaninol and (RS)- 2 – tetrahydrofurfuryl acid in an organic solvent in the 1st splitting obtained after reaction diastereoisomer salt, then re-crystallization (S)- 2 – tetrahydrofurfuryl acid crude product, the crude product obtained after treatment of high optical purity (S)- 2 – tetrahydrofurfuryl acid, its ee value>99%; combined split mother liquor and recrystallization of the mother liquor, containing the (R)- 2 – tetrahydrofurfuryl acid mixed solution of the, then in the mixed solution of (R)- 2 – tetrahydrofurfuryl acid with D – phenylalaninol reaction into a salt, said salt by re-crystallization (R)- 2 – tetrahydrofurfuryl acid crude product, crude product after treatment to obtain the high optical pure (R)- 2 – tetrahydrofurfuryl acid, its ee value>99%. The invention to optical pure c serinol two configuration effectively split the 2 – tetrahydrofurfuryl acid, respectively shall be 2 – tetrahydrofurfuryl acid of the two kinds of optical isomers, its ee value is greater than 99%, secondly this invention is adopted as the solvent is cheap and low boiling point of acetone, ethyl acetate and the like solvent, are used as the split reaction and re-crystallization of the solvent, the solvent is easy to recovery and high recovery rate. (by machine translation)

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

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The emergence of drug-resistant strains of influenza virus makes exploring new classes of inhibitors that target universally conserved viral targets a highly important goal. The influenza A viral genome is made up of eight single-stranded RNA-negative segments. The RNA promoter, consisting of the conserved sequences at the 3? and 5? end of each RNA genomic segment, is universally conserved among influenza A virus strains and in all segments. Previously, we reported on the identification and NMR structure of DPQ (6,7-dimethoxy-2-(1-piperazinyl)-4-quinazolinamine) (compound 1) in complex with the RNA promoter. Here, we report on additional screening and SAR studies with compound 1, including ex vivo anti-influenza activity assays, resulted in improved cellular activity against influenza A virus in the micromolar range.

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

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Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.

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

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Alpha substituted carboxylic acids of formula (I): wherein R’ and R2 are as defined in the specification and R3 is A) formula (II); B) formula (III); C) formula (IV); and D) formula (V); wherein Y, Art, Are, AP, R4, R5, R6, R7, R6, R9, R9a, R10, R”, R12, R17, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR alpha/y related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders. ”

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

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Decarboxylative coupling of carboxylic acids with activated olefins has been accomplished using visible light photoredox catalysis. The strategic placement of a radical-stabilizing aromatic group at the beta-position of the olefin component biases the regioselectivity of the addition, allowing reliable, facile access to anti-Michael-type products from readily available precursors. The scope of this methodology was demonstrated with a range of carboxylic acids and appropriately substituted olefins and was applied toward a two-step synthesis of the antiarrhythmic agent encainide.

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

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Closely related structural analogues of prazosin have been synthesised and tested for inhibition and activation of Transport-P in order to identify the structural features of the prazosin molecule that appear to be necessary for activation of Transport-P. So far, all the compounds tested are less active than prazosin. It is shown that the structure of prazosin appears to be very specific for the activation. Only quinazolines have been found to activate, and the presence of the 6,7-dimethoxy and 4-amino groups appears to be critically important.

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

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The ability of the hydrosoluble ruthenium(ii) complexes [RuCl 2(eta6-arene)(PTA)] 3a-d, [RuCl2(eta 6-arene)(PTA-Bn)] 4a-d, [RuCl2(eta6-arene) (DAPTA)] 5a-d, [RuCl2(eta6-arene)(TPPMS)] 6a-d (arene = C6H6, p-cymene, 1,3,5-C6H3Me 3, C6Me6) to promote the atom-economic formation of beta-oxo esters, by addition of carboxylic acids to terminal propargylic alcohols in water has been explored. Scope, limitations and catalyst recycling have been evaluated using the most active catalyst [RuCl 2(eta6-C6H6)(TPPMS)], 6a.

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

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A new series of dihydrofolate reductase (DHFR) inhibitors, the 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines, were designed and optimized for antibacterial potency and enzyme selectivity. The most potent inhibitors in this series contained a five-membered heterocycle at the 2-position of the benzimidazole, leading to highly potent and selective compounds that exploit the differences in the size of a binding pocket adjacent to the NADPH cofactor between the bacterial and human DHFR enzymes. Typical of these compounds is 7-((2-thiazol-2-yl)benzimidazol-1-yl)-2,4 diaminoquinazoline, which is a potent inhibitor of S. aureus DHFR (Ki = 0.002 nM) with 46700-fold selectivity over human DHFR. This compound also has high antibacterial potency on Gram-positive bacteria with an MIC versus wild type S. aureus of 0.0125 mug/mL and a MIC versus trimethoprim-resistant S. aureus of 0.25 mug/mL. In vivo efficacy versus a S. aureus septicemia was demonstrated, highlighting the potential of this new series.

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

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The invention belongs to the field of pharmaceutical chemicals, and in particular relates to 2 – sulfur […] diketone derivatives and their use for medicine. Strictly speaking, the invention relates to the compounds of inhibiting poly (ADP – ribose) polymerase activity of the use, the enzyme also called poly (ADP – ribose) synthase and poly ADP – phosphoribosyl transferase, commonly referred to as PARP. The compounds of the invention have the following characteristics: Formula (1) compound, said A and D together can be substituted fused aromatic ring; X can beNRXorCRXRY;if X isNRX, is n is 1 or 2; if X isCRXRY, is n is1;RXcan be selected from H, can be substitutedC1-20hydrocarbyl, C5-20aryl, C3-20heterocyclic radical, an amido group, thio amide, ester, acyl and sulfonyl;RYfrom H, hydroxy, amino; orRXandRYjointly constitute the spiro-C3-7ring hydrocarbyl or heterocyclyl;R2andR3are H, or whenX=CRXRYwhen, R2, R3, RXandRYand they are connected together with a carbon atom can be of the aromatic ring can be substituted copolymer;R1selected from H or halogen. (by machine translation)

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Tetrahydroisoquinoline – Wikipedia,
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The invention relates to compounds acting as antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I): Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold-induced and/or exacerbated- respiratory disorders, urological disorders, corneal disordes associated to disturbances in the production of the tears and/or altered blinking such as epiphora and dry eye disease.

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