专利号:US-5338851-A 优先权日:1993-03-31 标 题:Synthesis of cis-decahydroisoquinoline-3-carboxylic acids 发明人:HUFF BRET E; KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C 权利人:LILLY CO ELI 摘要:This invention provides a process for the synthesis of cis-decahydroisoquinoline-3-carboxylic acids and provides intermediates in the synthesis thereof.
专利号:US-6362009-B1 优先权日:1997-11-21 标 题 :Solid phase synthesis of heterocycles 发明人:MUNOZ BENITO; CHEN CHIXU 权利人:MERCK & CO INC 摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
专利号:US-5591867-A 优先权日:1992-12-04 标 题 :Synthesis of kainic acid 发明人:MONN JAMES A 权利人:LILLY CO ELI 摘要:This invention provides a process for preparing kainic acid and provides intermediates in the synthesis thereof.
专利号:US-5200526-A 优先权日:1987-04-27 标题:Syntheses of optically pure α-amino acids from 3-amino-2-oxetanone salts 发明人:ARNOLD LEE D; VEDERAS JOHN C 权利人:UNIV ALBERTA 摘要:A process for the preparation of optically pure α-amino acids comprising the nucleophilic ring-opening of 3-amino-2-oxetanone salts. N-Protected serine β-lactones are deprotected to form heretofore unknown 3-amino-2-oxetanone and its corresponding salts. In turn these previously unknown 3-amino-2-oxetanone salts may be used in the synthesis of other novel or rare stereochemically-pure free amino acids.
专利号:US-6448412-B1 优先权日:1995-07-31 标题:Methods for the preparation and characterization of multi-substituted fullerenes 发明人:MURPHY RANDALL B; WILSON STEPHEN R; LU QUING 权利人:SPHERE BIOSYSTEMS INC 摘要:The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the C n fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3 He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.
专利号:US-6245919-B1 优先权日:1996-06-28 标 题:Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors 发明人:SHINOZAKI HARUHIKO; TAGUCHI TAKEO; ISHIDA MICHIKO 权利人:SHINOZAKI HARUHIKO; TAGUSHI TAKEO; NIPPON CHEMIPHAR CO 摘要:A cyclopropylglycine derivative having the following formula:and an intermediate compound for the synthesis of the cyclopropylglycine derivative are novel compounds. The cyclopropylglycine derivative shows a selectivity higher than that of the known agonists to metabotropic L-glutamate receptors, and therefore is a metabotropic type agonist to L-glutamate which has excellent characteristics.