(S)-2-甲基-Cbs-恶唑硼烷置于水体系中,用77%的收率获得(S)-(+)-Alpha,Alpha-二苯基脯氨醇 参考文献:Asymmetric Synthesis Of (M)-2-Hydroxymethyl-1-(2-Hydroxy-4,6-Dimethylphenyl)Naphthalene Via A Configurationally Unstable Biaryl Lactone 标题:Asymmetric Synthesis Of (M)-2-Hydroxymethyl-1-(2-Hydroxy-4,6-Dimethylphenyl)Naphthalene Via A Configurationally Unstable Biaryl Lactone 摘要: Doi:10.15227/orgsyn.079.0072
专利号:US-7973171-B2 优先权日:2005-06-13 标题:Process for synthesis of dialkoxyorganoboranes 发明人:BURKHARDT ELIZABETH; ATKINS WILLIAM 权利人:BURKHARDT ELIZABETH; ATKINS WILLIAM 摘要:The invention relates to a process for the synthesis of dialkoxyorganoboranes, in particular to a process for the synthesis of dialkoxyorganoboranes by an ester exchange reaction. Moreover, the invention relates to a process for the synthesis of organo-oxazaborolidine catalysts (organo-CBS) and of trialkylboroxins. Furthermore, the invention relates to methods of using dialkoxyorganoboranes for the preparation of organo-CBS catalysts and in Suzuki-type coupling reactions.
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:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
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-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.
摘要:Mase, N., Science of Synthesis Knowledge Updates, (2013) 3, 379. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 244. 摘要:Zaidlewicz, M.; Pakulski, M. M., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 96. 摘要:Yliniemelä-Sipari, S. M.; Pihko, P. M., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 665. 摘要:MacMillan, D. W. C.; Watson, A. J. B., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 324.