CAS: 618385-01-6; Ethyl ((1R,3Ar,4Ar,6R,8Ar,9S,9As)-9-((E)-2-(5-(3-Fluorophenyl)Pyridin-2-yl)Vinyl)-1-Methyl-3-Oxododecahydronaphtho[2,3-C]Furan-6-yl)Carbamate

上下游产品

(3R,3As,4S,4Ar,7R,8Ar,9Ar)-7-Amino-4-[(E)-2-[5-(3-Fluorophenyl)-2-Pyridinyl]Ethenyl]-Decahydro-3-Methylnaphtho[2,3-C]Furan-1(3H)-One 618386-15-5

((1R,3Ar,4Ar,6R,8Ar,9S,9As)-9-Formyl-1-Methyl-3-Oxododecahydronaphtho[2,3-C]Furan-6-yl)Carbamic Acid Ethyl Ester置于lithium Diisopropyl Amide,硫酸,水体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.5H,以90%的收率获得产物沃拉帕沙
参考文献:Wo2006/76564
标题:Wo2006/76564

专利信息

专利号:US-8273790-B2
优先权日:2005-01-14
标 题:Exo-selective synthesis of himbacine analogs
发明人：THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D
权利人:THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D; SCHERING CORP
摘要:This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:

专利号:WO-2024220674-A1
优先权日:2023-04-18
标题:Timescale-guided microfluidic synthesis of polyphenol-iron iii network nanocapsules of hydrophobic drugs
发明人：YEO YOON; HAN BUMSOO; SHEN YINGNAN
权利人:PURDUE RESEARCH FOUNDATION
摘要:A scalable method of continuous microfluidic synthesis of tannic acid-iron III (TA-FeIII) network (TFN) nanocapsules of a hydrophobic drug; a scalable method of continuous microfluidic synthesis of epigallocatechin-3-gallate iron III (EGCG-FeIII) network, (EFN) nanocapsules; hydrophobic drug nanocapsules synthesized in accordance with the method; and a method of administering a hydrophobic drug to a patient in need thereof by administering to the patient the hydrophobic drug nanocapsules.

专利号:US-7626045-B2
优先权日:2005-01-14
标题:Synthesis of himbacine analogs
发明人：THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG
权利人:SCHERING CORP
摘要:The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. n An example of a step in the synthesis of such a himbacine analog is as follows:

专利号:EP-1853592-B1
优先权日:2005-01-14
标题:Synthesis of himbacine analogs
发明人：THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG
权利人:SCHERING CORP
摘要:The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)

专利号:US-8329905-B2
优先权日:2006-06-30
标 题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
发明人：YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K
权利人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K; MERCK SHARP & DOHME
摘要:This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: n nwherein R 9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R 11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X 2 is Cl, Br, or I; X 3 is selected from Cl and Br; and PdL n is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

专利号:US-8618314-B2
优先权日:2005-01-14
标 题 :Exo- and diastereo-selective synthesis of himbacine analogs
发明人：WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE
权利人:WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE; MERCK SHARP & DOHME
摘要:This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: