专利号:US-11427596-B2 优先权日:2019-07-19 标 题:Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications 发明人:CHELVAM VENKATESH; DUDHE PREMANSH; KRISHNAN MENA ASHA; SONAWANE AVINASH 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Embodiments herein provide fused-pyrido heterocycles such as azaindoles, carboline derivatives, furo[b]pyridines or furo[b]pyridine-isatin hybrids of Formula I.Embodiments also relate to a process for a synthesis of variety of complex pyrido-heterocycles The pyrido-heterocycles can be used for treating cancer (cervix, kidney, lung, breast and epidermal skin) and multi-drug resistant tuberculosis. These heterocycles can also be used as anti-biofilm agents against pathogenic strains, which will minimize the risk of secondary infections.
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-2024294462-A1 优先权日:2023-02-15 标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate 发明人:SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD 权利人:NANOVATION THERAPEUTICS INC 摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-6013829-A 优先权日:1996-02-05 标 题 :Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl -3- phenyl propanoic acid, application to the synthesis of N-(mercaptoacyl) amino acid derivatives 发明人:DANVY DENIS; MONTEIL THIERRY; DUHAMEL PIERRE; DUHAMEL LUCETTE; LECOMTE JEANNE-MARIE; SCHWARTZ JEAN-CHARLES; NOEL-LEFEBVRE NADINE; GROS CLAUDE; PLAQUEVENT JEAN-CHRISTOPHE 权利人:BIOPROJET SOC CIV 摘要:PCT No. PCT/FR97/00218 Sec. 371 Date Nov. 26, 1997 Sec. 102(e) Date Nov. 26, 1997 PCT Filed Feb. 4, 1997 PCT Pub. No. WO97/29086 PCT Pub. Date Aug. 14, 1997Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in: a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride; b) preparing the monoacetates (VII R) or (VII S) respectively; c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R); d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R); e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R1SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).
专利号:WO-2025115036-A1 优先权日:2023-11-29 标题:A process for the synthesis of 2-(4-chlorophenyl)-2-hydroxy-n-(3-methoxy-4-(prop-2- yn-1-yloxy)phenethyl)acetamide, a key intermediate of mandipropamid 发明人:DEB INDUBHUSAN; MONDAL IMTIAJ; NASKAR KOUSHIK; ROY SHANTONU 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides an improved method for the preparation of building blocks 2- (4-chlorophenyl)-2-hydroxy-N-(3-methoxy-4-(prop-2-yn-1-yloxy)phenethyl)acetamide, a key intermediate for the synthesis of Mandipropamid. An efficient, safe, cost-effective method for the preparation of Mandipropamid is developed. The method involves simple Nitro-aldol reaction, LAH reduction and mild Amidation reaction for synthesizing key intermediate 2-(4- chlorophenyl)-2-hydroxy-N-(3-methoxy-4-(prop-2-yn-1-yloxy)phenethyl)acetamide (E). The current synthesis method of the invention has relatively simple operation, mild reaction conditions, high yield and a simple process with, a yield up to 90%. Subsequent product purification of this method uses filtration and crystallization methods and easy column chromatography separation. This approach is highly effective and scalable, contributing to both atom and step economy in the process Therefore, the research of its synthetic process has a wide range of applications from the drug development and material synthesis point of view.