Di-T-Butylphenylphosphine Borane Complex置于奎宁环体系中,用 甲苯 作为反应溶剂,化学反应生成 二叔丁基苯基膦 参考文献:路易斯碱离核参数 Nfb 及其在 Mida-硼酸盐水解动力学分析中的应用 标题:路易斯碱离核参数 Nfb 及其在 Mida-硼酸盐水解动力学分析中的应用 摘要:已经测量了从广泛的路易斯碱硼烷加合物中置换 Bh 3的奎宁环动力学.这些速率的参数化使得能够开发出离核量表 (Nf B),以量化和预测一系列其他路易斯碱基的离去基团能力.在多个系列 R' 3-N R N X (X = P,N; R' = 芳基,烷基) 中观测到的可加性允许制定相关的取代基参数 (N F Pb,N F Ab),提供了一种方法计算n F B一系列路易斯碱基的值远远超出了实验得出的值.通过取代基参数n F Pb与一系列烷基和芳基 Mida 硼酸盐在中性条件下的水解速率的相关性,探索了核离性参数的效用.这允许鉴定具有接近反应中心的杂原子的 Mida 硼酸盐,显示出不寻常的动力学不稳定性或水解稳定性. DOI:10.1021/acs.Joc.1C02729
专利号:US-11459549-B2 优先权日:2018-05-10 标 题:Method for biocatalytic synthesis of Sitagliptin and intermediate thereof 发明人:WU FAHAO; YANG WEN; LI GANG; SHI HONGWEI; GAO YANGZHE; LIU LILI; YUAN ZHIFA 权利人:CHINA FORTUNE WAY COMPANY; NANJING REDWOOD FINE CHEMICAL CO LTD 摘要:Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.
专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-10570114-B2 优先权日:2016-05-19 标题:Synthesis of 6-aryl-4-aminopicolinates and 2-aryl-6-aminopyrimidine-4-carboxylates by direct suzuki coupling 发明人:FISK JASON S; LI XIAOYONG; Muehlfeld Mark; BAUMAN ROBERT S; OPPENHEIMER JOSSIAN; TU SIYU; NITZ MARK A; CHAKRABARTI REETAM; FEIST SHAWN D; RINGER JAMES W; LENG RONALD B 权利人:DOW AGROSCIENCES LLC 摘要:Improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates and arylalkyl and alkyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates, are described herein. The improved methods include a direct Suzuki coupling step, which eliminates the protection/de-protection steps in the current chemical process, and therefore eliminates or reduces various raw materials, equipment and cycle time as well as modification of other process conditions including use of crude AP, use of ABA-diMe, and varying pH, catalyst concentration, solvent composition, and/or workup procedures. This includes synthesis of 2-aryl-6-aminopyrimidine-4-carboxylates.
专利号:US-2023174490-A1 优先权日:2020-03-18 标 题 :Improved synthesis of 6-aryl-4-aminopicolinates 发明人:ZHANG CHUNMING; TU SIYU; LENG RONALD B; IRVINE NICHOLAS; SCHUITMAN ABRAHAM; SHINKLE AARON; DEVARAJ JAYACHANDRAN; ZU CHENGLI 权利人:CORTEVA AGRISCIENCE LLC 摘要:The present disclosure relates to improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates.
专利号:US-9718807-B2 优先权日:2012-06-05 标 题 :Synthesis of antiviral compound 发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE 权利人:GILEAD PHARMASSET LLC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:WO-2018175954-A1 优先权日:2017-03-23 标 题 :Synthesis of imidazo[5,1-a]isoindole derivative useful as ido inhibitors 发明人:ANGELAUD REMY; BACHMANN STEPHAN; BEYELER ANDREAS; CARRERA DIANE; FISCHER ROLF; GUILLEMONT-PLASS MAUD; HOU HAIYUN; IDING HANS; KRAFT ANNE KATRIN; MANNS ANDREAS; MEIER ROLAND; NIEDERMANN KARIN; OLBRICH MARTIN; PIECHOWICZ KATARZYNA; REGE PANKAJ; REMARCHUK TRAVIS; SIROIS LAUREN; ST-JEAN FREDERIC; XU JIE 权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE; GENENTECH INC 摘要:Presently provided is a method of making a compound of the Formula (I) wherein X is halogen, which is useful for modulating the activity of indoleamine 2,3-dioxygenase (IDO) and treating diseases and conditions in which the inhibition of IDO mediated immunosuppression is beneficial.