四氢吡喃,乙酸酐置于magnesium Bromide体系中,用 乙腈 用作溶剂,化学反应生成5-溴代戊基乙酸酯 参考文献:Cleavage Of Cyclic Ethers By Magnesium Bromide-Acetic Anhydride. Sn2 Substitution At A Secondary Site 标题:Cleavage Of Cyclic Ethers By Magnesium Bromide-Acetic Anhydride. Sn2 Substitution At A Secondary Site 摘要: Doi:10.1021/jo00912A022
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-3825607-A 优先权日:1972-01-17 标题 :Synthesis of 1-bromo-trans-3,trans-5-heptadiene 发明人:DESCOINS C; HENRICK C 权利人:ZOECON CORP 摘要:1-HALO-3,5-HEPTADIENE, PREPARED BY THE ACTION OF AQUEOUS HYDROPHALIC ACID ON 1-CYCLOPRROPYL-2-BUTEN-1-OL WHICH MAY BE PREPARED BY A GRIGNARD REACTION BETWEEN CROTONALDEHYDE AND CYCLOPROPYL MAGNESIUM HALLIDE OR BETWEEN CYCLOPROPYL CYANIDE AND 1-PROPYNYL MAGNESIUM HALIDE. IT IS USEFUL IN PREPARING 8.10-DODECADIENOL, A KNOWN CODLING MOTH SEX ATTRACTANT.
专利号:US-8044203-B2 优先权日:2002-05-10 标 题 :Chiral indole intermediates and their fluorescent cyanine dyes containing functional groups 发明人:MUJUMDAR RATNAKER B; WEST RICHARD MARTIN 权利人:UNIV CARNEGIE MELLON; GE HEALTHCARE UK LTD 摘要:This invention relates to the functionalized cyanine dyes and more particularly, to the synthesis of chiral 3-substituted 2,3′-dimethyl-3H-indole and its derivatives as intermediates for preparation of cyanine dyes, to methods of preparing these dyes and the dyes so prepared.
专利号:EP-0789577-B1 优先权日:1995-06-07 标 题:Synthesis of n-substituted oligomers
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 38. 摘要:Park, K.; Jo, H., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 916. 摘要:Geetharani, K.; Bose, S. K., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 348. 摘要:Adak, L.; Sahoo, S.; Aoki, S.; Kawanaka, Y.; Nakamura, M., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 408.