专利号:US-9126896-B2 优先权日:2012-06-01 标题:Synthesis of diamido gellants by using Dane salts of amino acids 发明人:BINDL MARTIN; HERRMANN ROLAND; KNAUP GUNTER 权利人:EVONIK INDUSTRIES AG 摘要:The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a Dane salt according to formula II and a Dane salt according to formula III with a coupling reagent; b) adding a diamine according to formula IV to the reaction mixture; and c) adding an acid to the reaction mixture to adjust the pH value of the reaction to <7; wherein L represents a C 2 -C 20 alkyl group, a C 6 -C 20 aryl group, or a C 7 -C 20 alkylaryl group; R 1 and R 2 can be identical or different and represent a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 hydroxyalkyl group, a C 1 -C 4 thioether group, a C 6 -C 20 aryl group, a C 7 -C 20 alkylaryl group, a C 7 -C 20 alkylhydroxyaryl group, a C 4 -C 20 alkylheteroaryl group with 1 to 4 heteroatoms; or a C 1 -C 4 alkylcarboxylic moiety, which may be an acid, an amide, or which may be esterified with a C 1 -C 6 alkyl group or a C 7 -C 20 alkylaryl group; R 3 represents a C 1 -C 4 alkyl group; R 4 represents a hydrogen atom, or a C 1 -C 4 alkyl group; R 5 represents a C 1 -C 4 alkyl group; and X represents an alkali metal.
专利号:US-5554725-A 优先权日:1994-09-14 标题:Synthesis of dolastatin 15 发明人:PETTIT GEORGE R 权利人:UNIV ARIZONA 摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.
专利号:US-9126897-B2 优先权日:2012-06-01 标 题 :Synthesis of diamido gellants by using amino acid N-carboxyanhydrides 发明人:BINDL MARTIN; HERRMANN ROLAND; KNAUP GUNTER 权利人:EVONIK INDUSTRIES AG 摘要:The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a N-carboxyanhydride according to formula II and a N-carboxy-anhydride according to formula III with a diamine according to formula IV and b) adding an acid to the reaction to adjust the pH value of the reaction to <7; wherein L represents a C 2 -C 20 alkyl group, a C 6 -C 20 aryl group, or a C 7 -C 20 alkylaryl group; and R 1 and R 2 can be identical or different and represent a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 hydroxyalkyl group, a C 1 -C 4 thioether group, a C 6 -C 20 aryl group, a C 7 -C 20 alkylaryl group, a C 7 -C 20 alkylhydroxyaryl group, a C 4 -C 20 alkylheteroaryl group with 1 to 4 heteroatoms; or a C 1 -C 4 alkylcarboxylic moiety, which may be an acid, an amide, or which may be esterified with a C 1 -C 6 alkyl group or a C 7 -C 20 alkylaryl group.
专利号:US-7189849-B2 优先权日:1997-02-10 标 题:Synthesis of acyclic nucleoside derivatives 发明人:LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY 权利人:MEDIVIR AB 摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.
专利号:US-4504415-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 and desacetyl thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.
专利号:US-4517119-A 优先权日:1983-04-04 标题:Synthesis of thymosin α1 发明人:FELIX ARTHUR M; GILLESSEN DIETER; LERGIER WILLIAM; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD 权利人:HOFFMANN LA ROCHE 摘要:An improved solution phase synthesis of thymosin α 1 and proceeding through novel intermediates is disclosed.
摘要:Ghosh, B.; Maleczka, R. E., Jr., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 355. 摘要:Lai, J.; Thomson, B. J.; Sammis, G. M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 38.