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磷酰基乙酸三乙酯置于sodium Hydroxide体系中,化学反应生成 二乙基磷乙酸
参考文献:Synthesis Of Orthogonally Protected (2S)-2-Amino-Adipic Acid (α-Aaa) And (2S,4R)-2-Amino-4-Hydroxyadipic Acid (Ahad)
标题:Synthesis Of Orthogonally Protected (2S)-2-Amino-Adipic Acid (α-Aaa) And (2S,4R)-2-Amino-4-Hydroxyadipic Acid (Ahad)
摘要:(2S,4R)-2-氨基-4-羟基己二酸(ahad)结构单元45由市售材料经11步反应,6.5%的整体收率合成.手性控制的关键步骤包括采用脯氨酸基催化剂进行的不对称共轭加成,以及氧亲核试剂对α,β-不饱和酯的syn选择性分子内共轭加成.为了实现α-氨基己二酸(α-Aaa)和ahad在肽中的掺入,开发了一种真正正交的保护基方案:包括用于n-端的烯丙氧基羰基(alloc)碳酸酯,用于δ-羧酸的叔丁氧基酯,用于α-羧酸的乙酰氧基酯以及用于ahad中γ-羟基的叔丁基二甲基硅醚保护基.
DOI:10.1021/jo400558T

专利信息

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-9242965-B2
优先权日:2013-12-31
标题:Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
发明人：ZHENG JUNCHENG; DENG DA; LV GUANGHUA; YAN JUN; BRANDENBURG JOERG; KROEBER JUTTA; SCHOLZ ULRICH
权利人:BOEHRINGER INGELHEIM INT
摘要:The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I n nwherein R 1 and R 2 independently denote C 1-3 -alkyl groups and X − denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.

专利号:US-6765114-B1
优先权日:1998-12-29
标题 :Process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid
发明人：GIZUR TIBOR; LENGYEL ZOLTANNE; SZALAI KRISZTINA
权利人:RICHTER GEDEON VEGYESZET
摘要:The invention relates to a new process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid of formula (I) via the new intermedier 1-(nitromethyl)cyclohexyl-acetic acid derivative of formula (II), wherein R represents hydrogen, benzyl group, diphenylmethyl group or C 1 -C 4 alkyl or alkoxy aromatic ring substituted derivatives thereof.

专利号:US-6710208-B2
优先权日:1996-12-19
标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARMA INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-11530204-B2
优先权日:2019-09-30
标 题 :Biocatalytic synthesis of cryptophycin anticancer agents
发明人：SHERMAN DAVID H; SCHMIDT JENNIFER J
权利人:UNIV MICHIGAN REGENTS
摘要:The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.

专利号:US-2005027143-A1
优先权日:2001-08-24
标 题 :Process for the preparation of beta-ionylideneacetaldehyde
发明人：SALMAN MOHAMMAD; RAY PURNA CHANDRA; BABU SURESH JAYACHANDRA; KUMAR NARESH
摘要:The present invention relates to an industrially advantageous process for the preparation of beta-ionylidencacetaldehyde of structural Formula I, which is a key intermediate for the synthesis of vitamin A and related compounds such as tretinoin and isotretinoin.