专利号:US-10899773-B2 优先权日:2014-12-19 标 题 :Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs 发明人:NICOLAOU KYRIACOS C; CAI QUAN 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
专利号:WO-2010144293-A1 优先权日:2009-06-08 标 题 :Synthesis of telcagepant and intermediates thereof 发明人:XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 权利人:MERCK SHARP & DOHME; XU FENG; DESMOND RICHARD; HOERRNER R SCOTT; HUMPHREY GUY R; ITOH TETSUJI; JOURNET MICHEL; YOSHIKAWA NAOKI; ZACUTO MICHAEL J 摘要:Disclosed is an efficient synthesis for the manufacture of the caprolactam intermediate (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one: Formula and salts thereof, and an efficient preparation of telcagepant using the caprolactam intermediate.
专利号:US-7820858-B2 优先权日:2006-03-25 标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation 发明人:CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.
专利号:US-9593071-B2 优先权日:2011-11-22 标题 :Process for the preparation of gamma amino acids and intermediates used in said process 发明人:ADAMO MAURO 权利人:ROYAL COLLEGE SURGEONS IRELAND 摘要:The invention relates to the preparation of gamma amino acids of formula (I) and pharmaceutically acceptable salts, solvates and prodrugs thereof, and to intermediates used for their preparation. (formula I) wherein R 1 is selected from an alkyl group, an alkenyl group, an alkynyl group and a cycloalkyl group, each of which may be optionally substituted and * denotes a chiral center. In particular, the present invention provides an efficient synthesis of (S)-pregabalin which is suitable for carrying out on an industrial scale.
专利号:US-8338620-B2 优先权日:2007-04-03 标 题:Methods for the production of C-8 lactam lactone compounds 发明人:SEDELMEIER GOTTFRIED 权利人:SEDELMEIER GOTTFRIED; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, the invention relates to a process for the manufacture of a compound of the formula I, n nor a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
专利号:US-2007276142-A1 优先权日:2004-02-19 标题 :Catalytic Asymmetric Synthesis of Optically Active Alpha-Halo-Carbonyl Compounds
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