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-11912654-B2 优先权日:2021-09-03 标 题:Process for stereospecific synthesis of vitamin K2 and its novel intermediates 发明人:MEHTA DILIP; SHASHTRI MAYANK; RAJU BNS; SHAH ASHWIN; VORA PARIN; MAHALE UMAKANT 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7. The present disclosure further discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.
专利号:WO-2023031841-A1 优先权日:2021-09-03 标题:A process for the stereospecific synthesis of vitamin k2 and its intermediates 发明人:MEHTA DILIP; SHASHTRI MAYANK; RAJU BNS; VORA PARIN; MAHALE UMAKANT 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7, in particular. It also discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.
专利号:US-11434211-B2 优先权日:2020-06-16 标题:Synthesis of 5-nitrotetrazole 发明人:PIERCEY DAVIN GLENN; MANSHIP TIMOTHY D; SMITH DAWSON MICHAEL 权利人:PURDUE RESEARCH FOUNDATION 摘要:This disclosure shows the ability of a readily-available oxidizer to achieve oxidation of 5-amino-1H-tetrazole (5-AT) to 5-nitrotetrazole (5-NT) in high yields in a single pot synthesis. This strategy reduces the synthesis of this important energetic material down to a single step and eliminates highly sensitive diazonium and copper salt primary explosive intermediates. The overall yield of this process is 48-53% and the resultant aqueous solution of product effectively used for the preparation of nitrotetrazole-containing primary explosive DBX-1. Unlike current methods of nitrotetrazole preparation, the novel method is entirely solution-based and prepares a final solution of sodium nitrotetrazolate, never once needing to handle energetic intermediates or products, making it a much safer method of nitrotetrazole preparation.
专利号:US-4592874-A 优先权日:1980-05-14 标 题:Process for the synthesis of alpha-chlorinated chloroformates 发明人:CAGNON GUY C; PITEAU MARC D; SENET JEAN-PIERRE G; OLOFSON ROY A; MARTZ JONATHAN T 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:Process for the synthesis of alpha -chlorinated chloroformates, and new alpha -chlorinated chloroformates. The invention relates to a new process for the manufacture of alpha -chlorinated chloroformates and, to new alpha -chlorinated chloroformates as new industrial products. The process according to the invention consists of a synthesis, by catalytic phosgenation, of alpha -chlorinated chloroformates of the formula: in which: R represents a substituted or unsubstituted hydrocarbon radical and m represents an integer superior or equal to one, this synthesis consisting in reacting phosgene with the aldehyde R-CHO)m, in the presence of a catalyst which is an organic or inorganic substance which is capable in a medium containing an aldehyde of the formula R-CHO)m, phosgene and, possibly, a solvent, of generating a pair of ions one of which is an halogenide anion and the other is a cation which is sufficiently separated from said halogenide anion so as to give to the latter a nucleophilic power enabling it to react with the function(s) aldehyde of the molecule R-CHO)m.
专利号:US-2011245503-A1 优先权日:2008-11-28 标题 :Enantioselective synthesis of asymmetric beta-carboline intermediates 发明人:SANTOS LEONARDO; ESPINOZA MORAGA MARLENE; SHANKARAJAH NAGULA 权利人:UNIV TALCA 摘要:Described herein is a new asymmetric synthesis of imines to obtain β-carboline derivatives useful as key intermediate compounds for the synthesis of phosphodiesterase inhibitors using a new process with palladium or ruthenium hydride and/or nickel boride to reduce chiral intermediates. The use of chloroformate chiral auxiliaries is further described for the reduction and asymmetric hydrogenation of imines to obtain β-carboline derivatives and intermediate compounds used in the preparation thereof.
参考文献:10.1002/anie.201103028 摘要:Spisak SN, Zabula AV, Filatov AS, Rogachev AY, Petrukhina MA. Selective endo and exo binding of alkali metals to corannulene. Angew Chem Int Ed Engl. 2011 Aug 22;50(35):8090–4. doi: 10.1002/anie.201103028. 参考文献:10.1107/s1600536811009299 摘要:Dhifet M, Belkhiria MS, Daran J, Nasri H. Chlorido{5,10,15,20-tetrakis[2-(2,2-dimethylpropanamido)phenyl]porphyrinato-κ4N,N′,N′′,N′′′}iron(III) chlorobenzene hemisolvate monohydrate. Acta Crystallogr E Struct Rep Online. 2011 Mar 15;67(4):m460–1. doi: 10.1107/s1600536811009299. 参考文献:10.1107/s1600536811007082 摘要:Wang WZ, Li XJ, Wang N. Benzyl-aminium perchlorate-18-crown-6 (1/1). Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o772. 参考文献:10.1107/s1600536811013997 摘要:Gaertner S, Korber N. [Rb(18-crown-6)][Rb([2.2.2]-cryptand)]Rb2Sn9·5NH3. Acta Crystallogr E Struct Rep Online. 2011 Apr 22;67(5):m613–4. doi: 10.1107/s1600536811013997. 参考文献:10.1007/s10337-011-1960-3 摘要:Studzińska S, Molíková M, Kosobucki P, Jandera P, Buszewski B. Study of the Interactions of Ionic Liquids in IC by QSRR. Chromatographia. 2011 Feb 25;73(Suppl 1):35–44. doi: 10.1007/s10337-011-1960-3.