CAS: 80-58-0; 2-Bromobutanoic Acid

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2681-94-9 32659-49-7 24457-21-4

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L-2-氨基丁酸置于氢溴酸,Sodium Nitrite体系中,用 水 作为反应溶剂,化学反应生成 S-2-溴丁酸
参考文献:铝催化二硫内酯开环聚合制备具有性能优势的立规可回收塑料
标题:铝催化二硫内酯开环聚合制备具有性能优势的立规可回收塑料
摘要:铝络合物与硫化物增长物质具有适当的结合亲和力,可避免催化剂中毒并最大限度地减少差向异构化反应.通过适当的配体设计和修饰,铝催化剂能够生产高度全同立构的立体络合聚硫酯.获得的二硫内酯基塑料是一种坚韧的半结晶材料,具有完全的可回收性.
DOI:10.1002/anie.202302898

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:WO-2015183067-A1
优先权日:2014-05-30
标题 :Synthesis of analogues of y-amino acids and resulting products
发明人：FERNÃ?NDEZ ZERTUCHE MARIO; TOVAR GUDIÑO ERIKA; TRUJILLO FERRARA JOSÉ GUADALUPE; GUEVARA SALAZAR JUAN ALBERTO
权利人:UNIV AUTÓNOMA DEL ESTADO DE MORELOS
摘要:The invention relates to a compound of formula (see formula), suitable for use as drugs in the treatment of chronic neurodegenerative disorders of the Huntington's disease, Parkinson's disease and epilepsy type, inter alia . The invention relates to novel methods for the synthesis of said analogues and the pharmaceutically acceptable solvates and salts thereof.

专利号:US-6172226-B1
优先权日:1993-12-22
标 题:Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions
发明人：COULL JAMES M; EGHOLM MICHAEL; HODGE RICHARD P; ISMAIL MOHAMED; RAJUR S B
权利人:PERSEPTIVE BIOSYSTEMS INC
摘要:A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.

专利号:US-2023148151-A1
优先权日:2020-04-17
标 题 :Process for the synthesis of a conjugate of hyaluronic acid and paclitaxel
发明人：CAMPISI MONICA; GUARISE CRISTIAN; PIZZOCARO CARLO
权利人:FIDIA FARM SPA
摘要:An industrial synthesis process of a hyaluronic acid-paclitaxel conjugate obtained by introducing the 4-bromobutyric acid spacer/linker between the hyaluronic acid and the paclitaxel, said conjugate being characterized by a high purity, the related pharmaceutical compositions for use in the treatment of multiple cancer forms are described.

专利号:US-5990341-A
优先权日:1993-11-08
标 题 :Diastereoselective synthesis hydroxyethylene dipeptide isosteres
发明人：LIOTTA DENNIS C; LAGU BHARAT RAMKRISHNA
权利人:UNIV EMORY
摘要:A process for the synthesis of hydroxyethylene dipeptide isosteres from α-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.

专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人：CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.