专利号:US-2024409495-A1 优先权日:2021-10-20 标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts 发明人:JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI 权利人:COUNCIL SCIENT IND RES 摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:WO-2025119975-A1 优先权日:2023-12-04 标 题:A method for synthesis of harmine 发明人:HETT ROBERT; GRAB HANUSCH; LAGOUTTE ROMAN 权利人:RECONNECT LABS AG 摘要:The invention relates to a method of synthesis of a compound of formula (I), harmine, according to the method comprising a step of transforming the compound of formula (II), into the compound of formula (I). The invention further relates to a compound of formula (II), which is an intermediate in synthesis of harmine according to the present invention.
专利号:WO-2004037772-A1 优先权日:2002-10-22 标 题 :Convenient and scalable synthesis of ethyl n-[(2-boc-amino) ethyl] glycinate and its hydrochloride salt 发明人:HUDSON ROBERT H E; VIIRRE RUSSELL D 权利人:UNIV WESTERN ONTARIO; HUDSON ROBERT H E; VIIRRE RUSSELL D 摘要:The present invention discloses an improved synthesis of ethyl N-[(2-Boc-amino)ethyl]glycinate and its hydrochloride salt. The synthesis is based on the reductive alkylation of Boc-ethylenediamine with ethyl glyoxylate hydrate and furnishes the title compound in near quantitative yield and high purity without chromatography. This compound is suitable, as is, for the synthesis peptide nucleic acid monomers. Further, conversion to the hydrochloride salt provides a stable, non-hygroscopic solid that is a convenient form for handling and storage.
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-11655264-B2 优先权日:2015-11-25 标题:Metallocene compounds, and preparation and use thereof for synthesis of poly-alpha-olefins as lubricating base oil 发明人:WEI DONGCHU; LI BING 权利人:APALENE TECH CO LTD JIAXING 摘要:The present invention relates to a metallocene compound, and preparation and use thereof, and the compound can be used as a catalyst for synthesis of poly-α-olefin as lubricating base oil. The metallocene compound includes a substituted aryl group, a bridged atom, an optionally unsubstituted, 3-mono-substituted or 3,6-disubstituted 5H-indeno [1,2-b] pyridyl group or optionally unsubstituted, 3-mono-substituted or 3,6-disubstituted 5H-indeno [1,2-b] thiopyranyl group, and a metal coordination group. As a catalyst, the metallocene compound is shown to be structurally stable and high in catalytic efficiency, and the preparation of the catalyst is relatively easy in operation, high in yield, low in cost, low in pollution and easy to scale up for industrial production.