专利号:US-2006074259-A1 优先权日:2004-10-01 标 题:Process for the enzymatic synthesis of pyroglutamic esters 发明人:PASCALY MATTHIAS; THUM OLIVER 权利人:GOLDSCHMIDT GMBH 摘要:A process for the preparation of compounds according to the general formula (I), n nin which R is a hydrocarbon radical of an alcohol, wherein one or more alcohols of the general formula (II) n nR—OH  (II)n nin which R is as defined above, are esterified and/or transesterified without using significant amounts of solvents, preferably without solvents, preferably under reduced pressure at temperatures below 100° C. in the presence of enzymes from the class of hydrolases with a compound according to the general formula (III), n n nin which R 1 is either hydrogen or a linear or branched alkyl or alkenyl group having 1 to 3 carbon atoms is provided.
专利号:US-8143416-B2 优先权日:2004-08-31 标题 :Alternative synthesis of renin inhibitors and intermediates thereof 发明人:SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH 权利人:SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH; NOVARTIS AG 摘要:The present invention relates to synthetic routes to prepare a compound of the formula n nwherein R 1 is halogen, C 1-6 halogenalkyl, C 1-6 alkoxy-C 1-6 alkyloxy or C 1-6 alkoxy-C 1-6 alkyl; R 2 is halogen, C 1-4 alkyl or C 1-4 alkoxy; R 3 and R 4 are independently branched C 3-6 alkyl; and R 5 is cycloalkyl, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkanoyloxy-C 1-6 alkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, C 1-6 dialkylamino-C 1-6 alkyl, C 1-6 alkanoylamino-C 1-6 alkyl, HO(O)C—C 1-6 alkyl, C 1-6 alkyl-O—(O)C—C 1-6 alkyl, H 2 N—C(O)—C 1-6 alkyl, C 1-6 alkyl-HN—C(O)—C 1-6 alkyl or (C 1-6 alkyl) 2 N—C(O)—C 1-6 alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
专利号:EP-3174849-B1 优先权日:2014-07-30 标 题:Synthesis of pyrrolidine derivatives
专利号:US-2008058528-A1 优先权日:2006-07-20 标题 :Synthesis of (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile
专利号:US-4975441-A 优先权日:1988-03-23 标 题:Lactams, their synthesis and use in cosmetic compositions 发明人:GIBSON WALTER T 权利人:UNILEVER PATENT HOLDINGS 摘要:A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises: (i) a chemical inhibitor of glycosidase activity chosen from lactams having the structure: where A<1> and A<6> are -H, -CH3, - @@0, -CH2OT or @@@0 A<1> and A<6> being the same or different, and at least one of which being the group: @ @@o in a lactam ring; and where Q is -OT min , -NHT min or a lactam linkage to A<1> or A<6>; the Q groups being the same or different, and at least one of which is involved in a lactam linkage; and where T is the same or different and is chosen from -H, -CpH2p+1 or a metal ion, T min is -H or -COCpH2p+1, and p is an integer of from 1 to 22; provided that: where any of the Q groups is -OT min or -NHT min , then that group or groups can be of either stereochemical configuration with respect to the plane of the ring; and (ii) a cosmetically acceptable vehicle for the chemical inhibitor. Certain novel lactams are also claimed.
专利号:CA-2657930-A1 优先权日:2006-07-20 标 题 :Synthesis of (2s,5r)-5-ethynyl-1-{n-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile
[参考文献]: Kim Kh, Et Al. 1-Carbomethoxy-β-Carboline, Derived From Portulaca Oleracea L., Ameliorates Lps-Mediated Inflammatory Response Associated With Mapk Signaling And Nuclear Translocation Of Nf-κb.Molecules. 2019 Nov 7;24(22). Pii: E4042.
合成参考文献
摘要:Elliott, M. C.; Jones, D. H., Science of Synthesis: Multicomponent Reactions, (2013) 2, 263. 摘要:Sasano, Y.; Iwabuchi, Y., Science of Synthesis: Special Topics, (2022) 1, 349.