专利号:US-7323575-B2 优先权日:2003-04-09 标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid 发明人:SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.
专利号:WO-9624694-A1 优先权日:1995-02-10 标 题:Method and kit for fluorometric analysis of enzymes catalyzing synthesis of nucleic acids 发明人:CHAVAN SURENDRA J; PROCHASKA HANS J 权利人:SLOAN KETTERING INST CANCER 摘要:This invention provides a method for detecting in a sample an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. Also provided is a method for determining in a sample the activity of such an enzyme. This invention also provides a method for detecting an RNA-DNA heteroduplex in a sample which comprises contacting the sample with a suitable fluorophore which selectively binds to double-stranded DNA. This method for detecting an RNA-DNA heteroduplex may further comprise quantitatively determining detected RNA-DNA heteroduplex. This invention also provides a method for detecting in a sample en enzyme which catalyzes the synthesis of and RNA-DNA heteroduplex from a nucleic acid template, as well as a method of detecting the activity of such an enzyme in a sample. This invention further provides a method for detecting the viral load of HIV in a sample. Also provided is a method for diagnosing an HIV infection in a subject, and for monitoring the progression of an HIV infection in a subject. Also provided is a method for determining the viral load of HIV in a subject infected with HIV. This invention further provides a method for identifying whether a substance inhibits reverse transcriptase. Finally, this invention provides a kit for assaying an enzyme which catalyzes the synthesis of a double-stranded nucleic acid molecule from a nucleic acid template.
专利号:US-9126995-B2 优先权日:2011-11-08 标题:Method for catalytic asymmetric synthesis of optically active isoxazoline compound and optically active isoxazoline compound 发明人:TOYAMA KEN-ICHI; MORIYAMA YUJI; MATOBA KAZUTAKA; YAOSAKA MANABU; IKEDA EITATSU 权利人:NISSAN CHEMICAL IND LTD 摘要:There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an α,β-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-8476441-B2 优先权日:2009-01-29 标 题 :Intermediates in the enantioselective synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid 发明人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN 权利人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN; TRINITY COLLEGE DUBLIN 摘要:(S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration.
专利号:US-4431828-A 优先权日:1982-11-10 标题 :Regeneration of 6-fluoro-4-chromanone from by-products in the synthesis of sorbinil 发明人:CUE JR BERKELEY W; HAMMEN PHILIP D; MASSETT STEPHEN S 权利人:PFIZER 摘要:6-Fluoro-4-chromanone, a sorbinil intermediate, is regenerated from enantiomeric and mixtures of enantiomeric and racemic compounds obtained as major by-products in the synthesis of sorbinil. The regenerated intermediate is useful in the synthesis of additional sorbinil.
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合成参考文献
摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484 参考文献:10.1038/s41592-019-0358-2] 摘要:Tidwell, T. T., Science of Synthesis, (2006) 23, 36.