CAS: 1360457-46-0; 2-((3R,6S)-2-Hydroxy-3-(2-(Thiophen-2-yl)Acetamido)-1,2-Oxaborinan-6-yl)Acetic Acid

上下游产品

(3S,6R)-Tert-Butyl 3-(Tert-Butyldimethylsilyloxy)-6-(2-Thiophen-2-Yl-Acetylamino)-6-[(2S,6R)-2,9,9-Trimethyl-3,5-Dioxa-4-Boratricyclo[6.1.1.02,6]Decan-4-Yl]Hexanoate 1681053-97-3

📜2-噻吩乙酸置于盐酸,Nickel(II) Chloride Hexahydrate,三乙氧基硅烷,四丁基碘化铵,(S)-3-Amino-2-Benzyl-1,4-Diphenylbutan-2-Ol,N,N'-羰基二咪唑体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,N,N-二甲基乙酰胺,水 用作溶剂,化学反应 26.0H,反应生成法硼巴坦
参考文献:一种镍催化的不对称氢酰胺化制备手性α-氨基硼酸/硼酸酯的方法
标题:一种镍催化的不对称氢酰胺化制备手性α-氨基硼酸/硼酸酯的方法
摘要:本发明公开了一种镍催化的不对称氢酰胺化制备手性α‑氨基硼酸/硼酸酯的方法.在金属镍盐,手性配体,氢源,添加剂等作用下,使烯烃和酰胺化试剂溶于有机溶剂中进行反应,得到区域选择性和对映选择性优秀的手性α‑氨基硼酸/硼酸酯.本方法原料易得,催化剂简单,操作简便,利用本方法可以合成一系列含有手性α‑氨基硼酸/硼酸酯的药物(生物活性)分子,如vaborbactam.

专利信息

专利号:US-10669292-B2
优先权日:2014-05-05
标 题 :Synthesis of boronate salts and uses thereof
发明人：HECKER SCOTT; BOYER SERGE
权利人:REMPEX PHARMACEUTICALS INC
摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.

专利号:US-9249175-B2
优先权日:2008-09-05
标 题 :RNA monomers containing O-acetal levulinyl ester groups and their use in RNA microarrays
发明人：DAMHA MASAD; LACKEY JEREMY; MITRA DEBBIE; WICKENS MARVIN; CERRINA FRANCO; SOMOZA MARK
权利人:DAMHA MASAD; LACKEY JEREMY; MITRA DEBBIE; WICKENS MARVIN; CERRINA FRANCO; AKHTAR SAIMA A; SOMOZA MARK; ROYAL INST FOR THE ADVANCEMENT OF LEARNING MCGILL UNIVERSITY; WISCONSIN ALUMNI RES FOUND
摘要:The present invention is directed to RNA monomers comprising O-acetal levulinyl protecting groups at the 2′ and/or the 5′-hydroxy functionalities of the ribose moiety. Said monomers may be incorporated into oligoribonucleotides or RNA polynucleotides. Furthermore, the invention is directed to methods for the synthesis of said RNA monomers, oligoribonucleotides and RNA polynucleotides, as well as methods for their deprotection and methods for the use of said compounds and compositions comprising said compounds. In particular, such compounds and compositions comprising them are used in methods for light-directed synthesis of RNA microarrays.

专利号:US-7820858-B2
优先权日:2006-03-25
标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation
发明人：CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.

专利号:US-9969686-B2
优先权日:2014-08-05
标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

专利号:US-2023212216-A1
优先权日:2019-12-20
标 题:Synthesis of lactone derivatives and their use in the modification of proteins
发明人：MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
权利人:GENIE BIOTECH UK LTD
摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

专利号:US-8106031-B2
优先权日:2006-05-02
标题:Hydrolytically-resistant boron-containing therapeutics and methods of use
发明人：LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A
权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC
摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.