专利号:US-11866398-B2 优先权日:2018-05-15 标 题:Total synthesis of prostaglandin J natural products by stereoretentive metathesis 发明人:LI JIAMING; CHEN XU; AHMED TONIA S; STOLTZ BRIAN M; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).
专利号:US-11247977-B2 优先权日:2018-06-22 标题 :Compound and use thereof in synthesis of brivaracetam intermediate and crude drug 发明人:FENG YAN; WANG RUYONG; YE YIZHANG; ZHANG FENGSEN; GONG XUAN; WANG ZHONGHONG; KANG XINSHAN 权利人:FUJIAN HAIXI PHARMACEUTICALS CO LTD 摘要:The present application provides a compound in formula III, and further provides a use of the compound in the synthesis of a Brivaracetam intermediate and a crude drug, and a synthesis method. A raw material involved in the method of the present application is low in costs and easily available; (R)-4-propyl-dihydrofuran-2-ketone having high optical purity can be prepared; complicated separation and purification steps are avoided; costs are reduced, and the method is more applicable to industrial production.
专利号:US-6087512-A 优先权日:1996-09-18 标题:Process for preparation of glycidyl ether 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; YANAGIMOTO TETSUYA; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of a glycidyl ether which is characrelized in reacting an epoxy compound of the formula ##STR1## wherein X is halogen or sulfonyloxy in the presence of a fluoride salt, with an alcohol. According to the above method, glycigyl ethers or their optically active compounds important as intermediates for synthesis of medicines are easily obtained in good yield and especially the optically active compounds are obtained with highly optical purity.
专利号:US-6057476-A 优先权日:1996-09-18 标题:Process for the preparation of 3-amino-2-hydroxy-1-propyl ethers 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula ##STR1## wherein R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R 2 and R 3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom, n which is characterized in reacting an epoxy compound of the formula ##STR2## wherein X is halogen, in the presence of a fluoride salt, with an alcohol and then reacting an amine. n According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.
专利号:US-2009247618-A1 优先权日:2008-03-26 标题 :Process for preparation of benzo-fused heteroaryl derivatives 发明人:BALLENTINE SCOTT A; REANY LAURA 权利人:BALLENTINE SCOTT A; REANY LAURA 摘要:The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.
专利号:US-8604241-B2 优先权日:2009-01-29 标题:Method for synthesis of (1S, 2R)-milnacipran 发明人:NICOLAS MARC; HELLIER PAUL; DIARD CATHERINE; SUBRA LAURENT 权利人:NICOLAS MARC; HELLIER PAUL; DIARD CATHERINE; SUBRA LAURENT; PF MEDICAMENT 摘要:The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt 2 , wherein M represents an alkaline metal, or with NHEt 2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.