专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
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-12312325-B2 优先权日:2022-03-01 标 题:Methods and compounds useful in the synthesis of an AAK1 inhibitor 发明人:CHEN TAO; WU WENXUE; YAN JUN; ZENG XIANGLU; ZHAO MATTHEW MANGZHU 权利人:LEXICON PHARMACEUTICALS INC 摘要:Methods for the synthesis of (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and salts thereof are disclosed, as well as compounds useful therein.
专利号:WO-2025132814-A1 优先权日:2023-12-21 标 题:Novel synthesis of methyl-2-fluoroacrylate 发明人:BRUNKE JESSICA; FISCHER MICHAEL; WÖSSNER JAN STEPHAN 权利人:VIFOR INT AG 摘要:The present invention relates to novel synthesis methods of methyl 2-fluoroacrylate (MFA) which is a key precursor for the production of Veltassa® (Patiromer). The methods according to the invention are conducted by reacting an α-substituted β-hydroxy propionic acid derivative (I) via one or more intermediate steps involving one or more α-, β-substituted propionic acid derivatives (II) to obtain MFA (III).
专利号:US-2022081407-A1 优先权日:2020-09-11 标题 :Methods of preparing substituted indanes 发明人:STENGEL PETER J; XU RUI; SPENCER STACEY RENEE 权利人:PELOTON THERAPEUTICS INC 摘要:This application discloses methods for the synthesis of substituted indane analogs that modulate HIF-2α activity, as well as key intermediates produced thereby. The synthesis of 3-(((1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile was exemplified.
专利号:US-7572942-B2 优先权日:2004-03-05 标题 :Synthesis of carbon-labeled perfluoroalkyl compounds 发明人:SHTAROV ALEXANDER BORISOVICH; HOWELL JON LEE 权利人:DU PONT 摘要:Various 13 C and 14 C carbon labeled compoundsn nR f — b CF(U) y (T) z   Formula 1A orn nR f — b CF 2 b CF(U) y (T) z   Formula 1Bn nwhereinn R f is a linear or branched perfluoroalkyl radical Z(C m F 2m )—, m is 1, 3 to 20, or a mixture thereof; Z is F when m is 1, and Z is F, Cl, or H when m is 3 to 20 or a mixture thereof; b is 13 or 14; y is 1, and z is 0 or 1; andn when y and z are each 1, U is F, and T is selected from the group consisting of monovalent radicals —X wherein X is I or Br, —CH 2 —CH 2 —X, —CHâ•?CH 2 , —CH 2 —CH 2 —OH, —CH 2 —COOH, —CH 2 OH, — b CH 2 OH, —COOH, — b COOH, —O—CF(CF 3 )—C(O)F, —O—CF(CF 3 )—X, —SO 2 Y wherein Y is H, F or Cl, and —SO 3 H; and when y is 1, and z is 0, U is selected from the group n consisting of divalent radicals â•?CH—COOH, â•?CHâ€CH 2 —OH, and â•?O, are disclosed, and a process for their preparation which selectively introduces 13 C and 14 C carbon labels into a fluoroalkyl chain.