专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-2007287843-A1 优先权日:2004-04-07 标题 :Methods and Intermediates for the Synthesis of Delta-9 Tetrahydrocannabinol 发明人:CABAJ JOHN E; PARIZA RICHARD J; LUKESH JULIE M 权利人:CABAJ JOHN E; PARIZA RICHARD J; LUKESH JULIE M 摘要:Processes are disclosed for the synthesis of Delta-9 tetrahydrocannabinol which result in an improved Y-THC/Y-THC ratio, and intermediates are disclosed that may be used in the synthesis of Delta-9 tetrahydrocannabinol such that improved Y-THCIY-THC ratios are achieved. The intermediates may be cyclic compounds prepared from 2-Carene. There is also provided a scaleable process for the preparation of (+)-p-menth-2-ene-1,8-diol, another intermediate used in the synthesis of delta-9-tetrahydrocannibinol.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2016031800-A1 优先权日:2013-03-14 标 题:Synthesis of chiral kynurenine compounds and intermediates 发明人:TRETYAKOV ALEXANDER; DROUET KEITH E; SANDERS WILLIAM 权利人:VISTAGEN THERAPEUTICS INC 摘要:Provided are methods for the synthesis of compounds including chiral kynurenine compounds, intermediates useful for the synthesis thereof, and related compounds. For example, methods are provided for the synthesis of L-4-chlorokynurenine.
专利号:WO-2021035382-A1 优先权日:2019-08-23 标题:Method forcontinuous synthesis of 2-cyclopentene-1-one 发明人:HONG HAO; LU JIANGPING; BAO DENGHUI; YUAN LONG; WANG BO 权利人:LIAONING ASYMCHEM LABORATORIES CO LTD 摘要:Provided is a method for the continuous synthesis of 2-cyclopenten-1-one. The continuous synthesis method comprises: loading a catalyst in a continuous reaction device, then continuously conveying cyclopentene, an oxidant and a solvent into the continuous reaction device for an oxidation reaction, and continuously discharging 2-cyclopentene-1-one. In the presence of the catalyst and the solvent, cyclopentene is used as a starting material, and same is directly oxidized by the oxidant, which can avoid the generation of a large amount of halogen-containing three wastes; at the same time, the entire continuous synthesis process is carried out in the continuous reaction device, which can effectively inhibit the occurrence of safety risks during scale-up production; in addition, after the reaction is complete, the product system of the oxidation reaction can be simply concentrated to obtain the target product (2-cyclopenten-1-one). Thus, the purity (up to 98% and above) and separation rate (up to 79%) of the product are greatly improved, and production can be easily scaled up.
专利号:US-4351767-A 优先权日:1981-06-29 标题 :Synthesis of 24,25-dihydroxycholesterol 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:This invention relates to the synthesis of steroids which are useful for their biological activity or which may be converted to steroids which have such activity. More particularly, the invention pertains to the synthesis of 24,25-dihydroxycholesterol. It includes intermediate sterols of this synthesis and processes for their preparation.
参考文献:10.1107/s1600536811010920 摘要:Choi HD, Seo PJ, Son BW, Lee U. 5-Cyclo-pentyl-3-methyl-sulfinyl-2-phenyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1000. 参考文献:10.1107/s160053681101097x 摘要:Choi HD, Seo PJ, Son BW, Lee U. 5-Cyclo-hexyl-2-(4-fluoro-phen-yl)-3-isopropyl-sulfonyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1001. 参考文献:10.1107/s1600536811010981 摘要:Choi HD, Seo PJ, Son BW, Lee U. 1-Cyclo-hexyl-sulfinyl-2-methyl-naphtho-[2,1-b]furan. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1002. 参考文献:10.1107/s1600536811007215 摘要:Choi HD, Seo PJ, Son BW, Lee U. 3-Cyclo-hexyl-sulfonyl-5-isopropyl-2-methyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o749. 参考文献:10.1107/s1600536811007112 摘要:Choi HD, Seo PJ, Son BW, Lee U. 5-Cyclo-hexyl-3-(4-fluoro-phenyl-sulfin-yl)-2-methyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o768.