专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-11891351-B2 优先权日:2020-03-20 标 题 :Synthesis of capsaicin derivatives 发明人:LAGER ERIK 权利人:AXICHEM AS 摘要:The present invention relates to the synthesis of capsaicin derivatives, specifically to the synthesis of 6-heptyne derivatives of capsaicin.
专利号:US-4288608-A 优先权日:1978-06-01 标题:Synthesis of anthracyclines 发明人:JOHNSON FRANCIS; KIM KYOUNG S 权利人:RESEARCH CORP 摘要:There is provided a novel method of synthesizing certain heterocyclic quinones. In particular there is provided a novel and regiospecific synthesis of 9-acetyl-6,11-dihydroxy-4-methoxy-7,8,9,10-tetrahydronaphthacene-5,12-quinone (7,9-dideoxydaunomycinone) which is known intermediate in the synthesis of daunomycinone. There is also provided a method of preparing analogs of 7,9-dideoxydaunomycinone which thus provide for the preparation of known and desired analogs of daunomycinone. Daunomycinone is a known compound which is an intermediate in the preparation of the clinically accepted naturally-occurring antitumor antibiotics daunomycin and its derivitive adriamycin.
专利号:US-4870199-A 优先权日:1986-04-30 标题 :Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 发明人:CHEN KAU-MING; HARDTMANN GOETZ E; KAPA PRASAD K; LEE GEORGE T; LINDER JEROME; WATTANASIN SOMPONG 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Process for the synthesis of compounds of the formula in R[R*,S*] enantiomeric form, wherein each P1 is independently an hydroxy group-protecting group, and R2z is C1-4alkyl, benzyl or allyl, comprising, as a key step when R2z is R2x, the reaction of the compound of the formula in (S) enantiomeric form with a compound of the formula Mg &cir& +2 ((-)OOC-CH2-COOR2x)2 to obtain a compound of the formula in (S) enantiomeric form, and, as a key step when R2z is R2y, the reaction of a compound of the formula in (S) enantioimeric form with a compound of the formula Li(+)(-)CH2-COOR2y to obtain a compound of the formula in (S) enantiomeric form, wherein R2x is primary or secondary C1-4alkyl, benzyl or allyl, R2y is C1-4alkyl not containing an asymmetric carbon atom, and R3' is methyl or ethyl, processes for the synthesis of compounds of the formula comprising reacting a compound of the formula with the reaction product of a strong base and a compound of the formula optionally followed by, when R2z is allyl, cleavage of the allyl and P1 groups to obtain the corresponding compound of the formula wherein each R7 is methyl or ethyl, R is as defined in the specification, and each P1 independently and R2z are as defined above, and the compounds of the formula wherein R and each R7 are as defined above.
专利号:US-5945548-A 优先权日:1995-03-03 标题:Process for the synthesis of α-substituted acrylic acids and their application 发明人:DUHAMEL PIERRE; DUHAMEL LUCETTE; DANVY DENIS; MONTEIL THIERRY; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES 权利人:BIOPROJECT SOC CIV 摘要:Process for the synthesis of α-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
专利号:US-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
参考标题:Catalytic Enantioselective Synthesis Of Bicyclic Lactam N ,S -Acetals In One Pot By Cascade Transformations 作者:Kaiheng Zhang,Luca Deiana,Erik Svensson Grape,A. Ken Inge,Armando Córdova |发布日期:2019.8.7 摘要:A Versatile Strategy For The Enantioselective Synthesis Of Bicyclic Lactam N,S-Acetals By One-Pot Cascade Transformations Is Disclosed. The Transformation Of Readily Available Substrates Is Promote ...
合成参考文献
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