CAS: 10487-71-5; But-2-Enoyl Chloride

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625-35-4 33698-85-0 3350-78-5

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巴豆酸置于光气,N,N-二甲基甲酰胺体系中,用 二氯甲烷 用作溶剂,化学反应生成巴豆酰氯
参考文献:通过 Co(III) 催化 α,β-不饱和化合物与未活化烯烃的脱氢交叉偶联
标题:通过 Co(III) 催化 α,β-不饱和化合物与未活化烯烃的脱氢交叉偶联
摘要:通过钴催化乙烯基 C-H 活化,α,β-不饱和化合物与未活化烯烃发生氧化交叉偶联.用各种不同官能化的不饱和化合物和未活化的烯烃检查了本发明的催化反应.在这些反应中,以非常好至优异的收率制备了高价值的酰胺官能化丁二烯和茚酮.提出了一种可能的反应机制,涉及通过碱辅助去质子化途径进行定向烯属 C-H 活化.
Doi:10.1021/acs.Orglett.3C02095

专利信息

专利号:US-5877278-A
优先权日:1992-09-24
标题:Synthesis of N-substituted oligomers
发明人：ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA
权利人:CHIRON CORP
摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.

专利号:US-4412079-A
优先权日:1968-03-13
标题:Thiadiazole compounds and methods of using said compounds in agriculture
发明人：CEBALO TONY; WALDE ROBERT A
权利人:AIR PROD & CHEM
摘要:Novel thiadiazole compounds are disclosed which contain in the 5 position, C-linked moieties which are either acyclic hydrocarbon radicals or halogenated acyclic hydrocarbon radicals (in which case each halogen is independently selected from F, Cl and Br). These novel compounds also contain an exocyclic nitrogen in the 2 position, and some of them contain the exocyclic substituent: wherein R3 is a lower acyclic hydrocarbon radical and R4 is either H or a lower acyclic hydrocarbon radical. Synthesis of these compounds is disclosed, including synthesis of those which exhibit isomerism and/or tautomerism. Various of these compounds have various agricultural utilities (e.g. as herbicides, insecticides, acaricides and fungicides), each of them having at least one such biological utility. Methods of using these compounds in phytotoxic fungicidal, acaricidal and insecticidal applications are disclosed.

专利号:US-6608196-B2
优先权日:2001-05-03
标题 :Process for solid supported synthesis of pyruvate-derived compounds
发明人：WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L
权利人:GALILEO PHARMACEUTICALS INC
摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

专利号:WO-0046211-A1
优先权日:1999-02-04
标题:Method of synthesizing barbituric acid derivatives and their use for the synthesis of chemical libraries
发明人：MJALLI ADNAN M M
权利人:TRANSTECH PHARMA; MJALLI ADNAN M M
摘要:A support template of Formula (1).

专利号:US-5668164-A
优先权日:1996-07-12
标 题:Process for synthesis of chiral cis-and trans-3-amino-4 substituted pyrrolidine compounds
发明人：MA ZHENKUN; COOPER CURT S; FUNG ANTHONY K L; CHU DANIEL T
权利人:ABBOTT LAB
摘要:Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas: ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas: ##STR2## with the assistance of a streochemically directing chiral oxazolidinone moiety having the formula: ##STR3## wherein P, R and R 1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated add chloride, reaction with N-benzyl-N-(methoxymethyl)trimethyl-silylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.

专利号:US-8487094-B2
优先权日:2008-07-25
标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
发明人：FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA
权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT
摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).