专利号:US-2021323987-A1 优先权日:2018-08-20 标题:Methods for the Synthesis of Heteroatom Containing Polycyclic Aromatic Hydrocarbons 发明人:GARG NEIL K; DARZI EVAN R; BARBER JOYANN S; SUSICK ROBERT; CHARI JASON; SPENCE KATIE 权利人:UNIV CALIFORNIA 摘要:Methods for the synthesis of polycyclic aromatic hydrocarbons and synthesis platforms for performing such syntheses are provided. Methods and platforms are provided that allow for the synthesis of aza-polycyclic aromatic hydrocarbons by an expedient ring assembly. Methods and platforms allow for a modular approach to synthesis that provide multiple new C—C bonds in sequential pericyclic reactions, thus giving access to compounds with multiple axes of substitution.
专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:WO-2025215126-A1 优先权日:2024-04-12 标题:Synthesis of vidofludimus and its calcium salt 发明人:VITT DANIEL; IGLICAR PETRA; GEGE CHRISTIAN; Mühler Andreas; KOHLHOF HELLA; GRÖPPEL MANFRED 权利人:IMMUNIC AG 摘要:The invention relates to the process of preparation of 2-fluoro-4-(3-methoxyphenyl)aniline (3) as an intermediate. Said intermediate 2-fluoro-4-(3-methoxyphenyl)aniline (3) is obtained in a Suzuki coupling reaction from (3-methoxyphenyl)boronic acid (1) and 4-bromo-2-fluoro-aniline (2). The invention further relates to the synthesis of vidofludimus (5) from said intermediate 2-fluoro-4-(3-methoxy-phenyl)aniline (3) and from 1-cyclopentene-1,2-dicarboxylic anhydride (4). The invention further relates to the synthesis of vidofludimus calcium (6) from said vidofludimus (5) and from a calcium salt, preferably Ca(OH)2.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-8283476-B2 优先权日:2007-06-26 标 题:Transition metal catalyzed synthesis of 2H-indazoles 发明人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS 权利人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.
专利号:WO-2021033165-A1 优先权日:2019-08-21 标 题:Process for synthesis of pyrazolidinone compounds 发明人:MATHUR SUCHET SARAN; MHATRE HRIDAYNATH VISHWANATH; PEDHAVI VISHAL PARSHURAM 权利人:GHARDA CHEMICALS LTD 摘要:The present disclosure relates to a process for the synthesis of pyrazolidinone, particularly alkyl 2-(3-chloropyridin-2-yl)-5-oxo-pyrazolidine-3-carboxylate (pyrazolidinone) compound. The process of the present disclosure is simple, economical, and produces alkyl 2-(3-5 chloropyridin-2-yl)-5-oxo-pyrazolidine-3-carboxylate with a comparatively high yields.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 591. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 605. 摘要:Stará, I. G.; Starý, I., Science of Synthesis, (2010) 45, 902. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 598. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 599.