专利号:US-7202370-B2 优先权日:2003-10-27 标 题 :Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III 发明人:NAIDU RAGINA 权利人:CONOR MEDSYSTEMS INC 摘要:A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.
专利号:US-2003004337-A1 优先权日:2000-05-04 标 题 :Efficient lactam synthesis 发明人:JUNG KYUNG WOON; YOON CHEOL HWAN 摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a γ-lactam, in which an a-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh 2 (OAc) 4 , n n n by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.
专利号:US-6689890-B2 优先权日:2000-05-04 标 题:Efficient lactam synthesis 发明人:JUNG KYUNG WOON; YOON CHEOL HWAN 权利人:UNIV SOUTH FLORIDA 摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a gamma-lactam, in which an alpha-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh2(OAc)4,by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.
专利号:US-4536334-A 优先权日:1979-06-28 标题 :Preparation of β-lactam derivatives 发明人:SUNAGAWA MAKOTO; MATSUMURA HARUKI; INOUE TAKAAKI; HIROHASHI TOSHIYUKI 权利人:SUMITOMO CHEMICAL CO 摘要:A process for preparing a β-lactam derivative having a hydrogen atom on the nitrogen atom of the β-lactam ring, which comprises reacting a β-lactam derivative having a mono- or diarylmethyl group on the nitrogen atom of the β-lactam ring with an acid or ceric ammonium nitrate to cleave the bond between the nitrogen atom and the mono- or diarylmethyl group; and novel β-lactam derivatives useful as intermediates for the synthesis of pharmaceutical agents.
专利号:US-4734495-A 优先权日:1985-07-17 标 题 :Process and intermediates for beta-lactam antibiotics 发明人:EVANS DAVID A; SJOGREN ERIC B 权利人:HARVARD COLLEGE 摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.
专利号:US-4086423-A 优先权日:1973-10-12 标题 :Process for cephem synthesis 发明人:FIRESTONE RAYMOND A; RATCLIFFE RONALD W; CHRISTENSEN BURTON G 权利人:MERCK & CO INC 摘要:Cephalosporin antibiotics of the formula: ##STR1## are produced by cycloaddition of a glycine derivative of the formula ##STR2## with a thiazine derivative of the formula ##STR3##