专利号:US-3992439-A 优先权日:1972-04-17 标 题:Synthesis of prostaglandins of the 'one'-series 发明人:SCHAAF THOMAS K; COREY ELIAS J 权利人:PFIZER 摘要:In the synthesis of prostaglandins of the 'one' -series an alteration in the conventional reaction sequence avoids side reactions and provides an improved synthesis via a series of novel intermediates. In this improved synthesis the side chain at the 8 position is attached to the five membered ring before the side chain at the 12 position is attached.
专利号:EP-2666771-A1 优先权日:2012-05-24 标题 :Synthesis of Aminocyclopentanetriol Derivatives 发明人:STERK DAMJAN; CASAR ZDENKO 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor. nThe present invention provides in particular a process for the preparation of a compound of formula Vn ncomprising: na) providing a compound of formula IVn n, and nb) reducing the compound of formula IV with activated zinc in the presence of copper to give the compound of formula V.
专利号:US-5665598-A 优先权日:1994-04-13 标题:Synthesis of chiral N-protected-α-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent 发明人:ABOOD NORMAN A; NOSAL ROGER A 权利人:SEARLE & CO 摘要:A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with alpha -chymotrypsin provides N-Boc-L-propargylglycine in high yield.
专利号:US-2012094919-A1 优先权日:2009-03-16 标题 :Use of tripeptides 发明人:GRAEUB REMO; HEIDL MARC; IMFELD DOMINIK; MUELLER EIKE; WIKSTROEM PETER; ZIEGLER HUGO 权利人:GRAEUB REMO; HEIDL MARC; IMFELD DOMINIK; MUELLER EIKE; WIKSTROEM PETER; ZIEGLER HUGO 摘要:The present invention relates to the use of tripeptide derivatives for tightening, firming and/or moisturizing skin. Furthermore, the invention relates to a method for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue and/or proteoglycans by fibroblasts and/or keratinocytes such as in particular the synthesis of Hyaluronic acid and/or of the proteoglycans Decorin and/or Lumican.
专利号:US-11542244-B2 优先权日:2018-05-18 标题 :Synthesis of tipifarnib 发明人:REN PINGDA; DENG XIAOHU; MAI WANPING 权利人:KURA ONCOLOGY INC 摘要:Provided herein are methods of preparing a desired enantiomer 6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone, otherwise known as tipifarnib.
专利号:WO-2011082700-A1 优先权日:2010-01-05 标题 :A method for the preparation of 6,7-dimethoxy-1-[2-(4-trifluoromethylphenyl)ethyl]-3,4- dihydroisoquinoline 发明人:RADL STANISLAV; CERNY JOSEF 权利人:ZENTIVA KS; RADL STANISLAV; CERNY JOSEF 摘要:The invention relates to a method of preparing 6,7-dimethoxy-l-[2-(4-trifluoromethylphenyl) ethyl]-3,4-dihydroisoquinoline I by cyclization of substance III, wherein the R substituent is a C1-C4 alkyl group, under conditions of acidic catalysis, the acidic catalyst being a strong inorganic acid, polyphosphoric acid or phosphorus oxychloride. The compound of formula (I) represents the key intermediate of synthesis of almorexant. (Formulae (I), (III))