专利号:US-2017267706-A1 优先权日:2014-08-19 标 题:Method for the synthesis of heterocyclic hydrogen phosphine oxide 发明人:BRUYNEEL FREDERIC; NOTTE PATRICK PIERRE 权利人:STRAITMARK HOLDING AG 摘要:A method for the synthesis of a heterocyclic hydrogen phosphine oxide, having the general formula: n n n n n n n n n n wherein:n nR is a aliphatic or aromatic divalent group optionally including one or more heteroatoms and optionally having one or more substituents andn nX and Y are independently selected from —O—, —C(O)O— and —NR′—n nwherein R′ is a monovalent group optionally having one or more heteroatoms including the steps of:n na) forming a reaction mixture by mixing a compound having the general formula HX—R—YH and tetraphosphorus hexaoxide; andn nb) recovering the resulting compound comprising the heterocyclic hydrogen phosphine oxide.
专利号:EP-2589587-A1 优先权日:2011-11-04 标题:Synthesis of nitrogen substituted cyclopropanes 发明人:RASPARINI MARCELLO; TADDEI MAURIZIO; CINI ELENA; MINELLI COSIMA; TURNER NICHOLAS; HUGENTOBLER KATHARINA GLORIA 权利人:CHEMO IBERICA SA 摘要:The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans- cyclopropanamine ( 1 ), a key intermediate in the synthesis of Ticagrelor:n n The invention also relates to the processes for preparing said compounds or their salts and the use of said compounds as intermediates in preparing pharmaceutically active ingredients.
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-5157129-A 优先权日:1990-04-18 标题:Enantiospecific synthesis of s-(+)-5,6-dihydro-4-(r-amino)-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide 发明人:BLACKLOCK THOMAS J; JONES TODD K; GRABOWSKI EDWARD J J; MATHRE DAVID J; MOHAN JULIE J; SOHAR PAUL; ROBERTS F EDWARD; XAVIER LYNDON C 权利人:MERCK & CO INC 摘要:5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxide is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.
专利号:US-2025163020-A1 优先权日:2022-08-31 标 题:Chiral Synthesis of Nornicotine and Nicotine 发明人:STRAKOVÃ? KAROLÃ?NA; MÜLLER DOMINIK SIMON; VAN VEGTEN CORNELIS HENDRIK; ZELLER FLORIAN DANIEL; DEBNAR THOMAS 权利人:SIEGFRIED AG; CONTRAF NICOTEX TOBACCO GMBH 摘要:The present invention relates to a method of producing nornicotine through enantioselective hydrosilylation of myosmine and a composition produced thereby, as well as a composition comprising nornicotine and a catalyst, wherein the catalyst is an organic chiral Lewis base, and a catalyst. The present invention also relates to a method of producing nicotine or a salt thereof from myosmine through enantioselective hydrosilylation of myosmine to nornicotine and further reacting the nornicotine to nicotine or a salt thereof, and a composition produced thereby, as well as a composition comprising nicotine, or a salt thereof, and a catalyst, wherein the catalyst.
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.
摘要:Chciuk, T. V.; Flowers, R. A.; Flowers, R. A., Science of Synthesis Knowledge Updates, (2016) 2, 223. 摘要:Kayaki, Y.; Ikariya, T., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 106.