专利号:US-3846399-A 优先权日:1969-04-10 标题:Process for controlled stepwise synthesis of polypeptides 发明人:HIRSCHMANN R; DENKEWALTER R 权利人:MERCK & CO INC 摘要:The invention disclosed herein relates to a novel process for the controlled, stepwise synthesis of polypeptides and proteins. More particularly, it is concerned with a process for the rapid and efficient preparation of polypeptides in which multiple sequential steps are carried out without isolation of intermediate peptides. This process for the controlled stepwise synthesis of polypeptides involves reacting a starting amino acid or peptide (or derivative thereof) with an N-carboxy amino acid anhydride (or derivative thereof) in an aqueous medium under conditions of controlled pH such that the only amino group present in appreciable concentration in reactive form during the course of the reaction is the amino group in the starting amino acid or peptide.
专利号:US-3944619-A 优先权日:1976-02-20 标 题 :Synthesis of d-2-amino-1-butanol 发明人:SINGH BALWANT 权利人:AMERICAN CYANAMID CO 摘要:D-2-Amino-1-butanol, for the synthesis of ethambutol hydrochloride, d,d'-2,2'-(ethylenediimino)di-1-butanol dihydrochloride, is produced in high purity and good yields by the reaction of butene-1, a nitrile, preferably an excess of acetonitrile, and chlorine to form N-[1-(chloromethyl)propyl]acetimidoyl chloride which is hydrolyzed to dl-2-amino-1-butanol, which can be isolated as the hydrochloride, or free base, or a mixture, resolved with L(+)- tartaric acid and the d-2-amino-1-butanol reacted with ethylene dichloride and then hydrochloric acid to form ethambutol hydrochloride. A minimum of by-products which are conveniently split out permits the economical synthesis of a pharmaceutical grade product.
专利号:US-3978084-A 优先权日:1973-12-03 标题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and thiophene intermediates in this synthesis.
专利号:US-3979396-A 优先权日:1973-12-03 标 题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and dihydrothiophene intermediates in this synthesis.
专利号:US-4000169-A 优先权日:1975-01-27 标题 :Asymmetric synthesis of optically active compounds 发明人:CHAN KA-KONG; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:Asymmetric synthesis of optically active 3,7,11-trimethyl-dodecan-1-ol, an intermediate for producing optically active vitamin E, from isovaleraldehyde or prenal including intermediates in this synthesis.
专利号:US-4029647-A 优先权日:1973-12-03 标 题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and thiophene intermediates in this synthesis.