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-4895922-A 优先权日:1988-05-05 标 题 :Low temperature synthesis of polyesteramides 发明人:OGATA NAOYA 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention disclosed a process for the synthesis of polyesteramides. By utilizing the phosphorus containing catalyst systems of the present invention, such polyesteramides can be synthesized at relatively low temperatures. The present invention specifically discloses a process for the synthesis of a polyesteramide which comprises polymerizing at least one diamine, at least one diol, and at least one dicarboxylic acid in the presence of (1) at least one acid acceptor; (2) at least one halogenated organic compound; and (3) at least one phosphorus containing compound selected from the group consisting of (a) triphenylphosphine, (b) triphenylphosphine oxide, (c) triphenylphosphine sulfide, (d) polymeric agents having pendant diphenylphosphine groups, (e) silicon-phosphorus compositions which contain at least one divalent oxygen atom which is bonded directly to a tetravalent silicon atom and a trivalent or pentavalent phosphorus atom; (f) compounds with the structural formula (C 6 H 5 ) 3 P=N-R, wherein R is a hydrogen atom or an alkyl group containing from 1 to 10 carbon atoms; and (g) compounds with the structural formula (C 6 H 5 )PR 1 R 2 wherein R 1 and R 2 can be the same or different, wherein R 1 is selected from the group consisting of alkyl groups containing from 1 to 10 carbon atoms and phenyl groups, and wherein R 2 is an alkyl group containing from 1 to 10 carbon atoms.
专利号:US-6063919-A 优先权日:1998-08-14 标题:Process for the synthesis of exochelins 发明人:GAUDIOSO LARRY A; WEGLARZ MICHAEL A 权利人:KEYSTONE BIOMEDICAL INC 摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.
专利号:US-9957355-B2 优先权日:2013-06-12 标 题 :Device and method for synthesis of a polymer under separation of a gaseous substance 发明人:ZHU NING; STAMMER ACHIM; CLAUSS JOACHIM; KORY GAD 权利人:BASF SE 摘要:The invention relates to a device for synthesis of a polymer under separation of a gaseous substance. Said device comprises a reaction chamber ( 1 ), which has a top section ( 11 ), a middle section ( 12 ) and a bottom section ( 13 ), an inlet opening ( 2 ) which is arranged in the middle section ( 12 ), a first outlet opening ( 3 ) which is arranged in the bottom section ( 13 ), a second outlet opening ( 4 ) which is arranged in the top section ( 11 ), a first return opening ( 51 ), which is arranged in the bottom section ( 13 ), a second outlet opening ( 52 ), which is arranged under the top section ( 11 ), a distribution device ( 6 ), which is arranged between the top section ( 11 ) and the middle section ( 12 ), and a removal device ( 7 ) which is arranged to be movable along the top section ( 11 ). The invention further relates to a method for synthesis of a polymer which can be carried out in said device.
专利号:US-7241900-B2 优先权日:2002-02-12 标题 :Synthesis of indole thiazole compounds as ligands for the Ah receptor 发明人:DELUCA HECTOR F; GRZYWACZ PAWEL K; SICINSKI RAFAL R 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
专利号:US-2024383940-A1 优先权日:2021-03-31 标题 :Synthesis of trinucleotide and tetranucleotide caps for mrna production 发明人:ENDO ATSUSHI 权利人:MODERNA TX INC 摘要:Provided herein are methods of making trinucleotides and tetranucleotides for use as 5′ mRNA caps. The methods utilize a novel “top-down†strategy and provide for synthesis of oligonucleotides with higher yields and increased efficiency compared to traditional methods. A key step of the methods disclosed, herein can also be adapted to utilize a “one-pot†approach, resulting in an increase in the yield of the final oligonucleotide product.
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合成参考文献
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