CAS: 22348-32-9; Diphenyl-[(2R)-Pyrrolidin-2-Yl]Methanol

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5-氧代吡咯烷-2-羧酸乙酯置于硼烷体系中,用 四氢呋喃 用作溶剂,化学反应 24.0H,反应生成(R)-(+)-Alpha,Alpha-二苯基脯氨醇
参考文献:一种稳定且易于制备的催化剂,用于酮的对映选择性还原.多步合成的应用
标题:一种稳定且易于制备的催化剂,用于酮的对映选择性还原.多步合成的应用
摘要:我们最近描述了一种将酮催化对映选择性还原为手性仲醇的新方法.还原反应的化学计量试剂为硼烷(通常为0.6Molfmol酮),催化剂为手性氧氮杂硼烷如1(0.05-0.1Molfmol酮).优异的对映选择性,手性催化剂前身的易回收性,接近定量的收率,较短的反应时间(在 23oc 下为几分钟)以及产品绝对构型的可预测性有助于该 (Cbs') 工艺的出色效用.本文报告了该领域在改进实用性和重要应用方面的几项后续发展.与对空气和水分均敏感的 1 相比,B-甲基化恶唑硼烷2可在室温下储存在密闭容器中,并在空气中称重或转移.催化剂 2 也比催化剂 1 更容易制备. (S)-的反应
Doi:10.1021/ja00259A075

专利信息

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; MÃœLLER 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.