专利号:US-11891375-B2 优先权日:2021-07-26 标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates 发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
专利号:US-11274081-B2 优先权日:2016-05-30 标 题:Process for the synthesis of ivacaftor 发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.
专利号:WO-9118002-A1 优先权日:1990-05-16 标 题 :Nucleosides as synthones for rna-synthesis 发明人:ERDMANN VOLKER; SPRINZL MATHIAS; HENCO KARSTEN 权利人:DIAGEN INST MOLEKULARBIO 摘要:Nucleosides are disclosed having formula (I), in which, when B represents guanine or 8-haloguanine, R?1 is an amidine protecting group, in particular the dimethylaminomethylene group (DMM) at the N?2 position of the purine group; R?2 is an alkylsilyl group or methyl group or hydrogen (H); R?3 is a triethylammonium H-phosphonate group, a hydrogen atom or a phosphoramidite group; R?4 is a substituted trityl protecting group or H, or when B represents adenine or 8-azidoadenine, R?1 is an amidine protecting group, in particular the dimethylaminomethylene group (DMM) at the N?6 position of the purine group and R?2, R?3 and R?4 have the same meanings as when B represents guanine. These compounds are useful as synthones for the chemical synthesis of RNA. When the DMM-protected purine bases adenine and guanine are used, coupling yields above 95 % are obtained.
专利号:US-5639785-A 优先权日:1995-06-07 标 题 :Methods for the treatment of baldness and gray hair using isoflavonoid derivatives 发明人:KUNG PATRICK C 权利人:GLOBAL PHARMA LTD 摘要:The present invention relates to novel pharmaceutical compositions of isoflavanoid derivatives useful for the treatment of male pattern baldness and alopecia areata, and their use in promoting the conversion of gray hair to the original pigment in hair follicles. Also described herein are methods for the synthesis of isoflavanoid derivatives.
专利号:US-10975096-B2 优先权日:2014-06-20 标题 :Synthesis of polycyclic-carbamoylpyridone compounds 发明人:CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W 权利人:GILEAD SCIENCES INC 摘要:Methods of making compounds of Formula I are disclosed:
专利号:WO-2022127920-A1 优先权日:2020-12-18 标 题:Preparation method for and intermediate of 5'-nucleoside prodrug 发明人:SHEN JINGSHAN; HU TIANWEN; XIE YUANCHAO; ZHU FUQIANG 权利人:TOPHARMAN SHANGHAI CO LTD 摘要:Provided in the present invention are a preparation method for and an intermediate of a 5'-nucleoside prodrug. Specifically, provided in the present invention is a method for preparing a compound of formula VI. The method comprises the steps of: (a) reacting a compound of formula I and a compound of formula II to obtain a compound of formula III; (b) reacting the compound of formula III and reagent M to obtain a compound of formula IV; (c) reacting the compound of formula IV in the presence of reagent N to obtain a compound of formula V; and (d) reacting the compound of formula V with reagent O to obtain a compound of formula VI. The preparation method provided by the present invention has the advantages of having low costs, high yield, good product purity and the like, and is capable of achieving the efficient synthesis of 5'-nucleoside prodrugs.