专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-11434211-B2 优先权日:2020-06-16 标题:Synthesis of 5-nitrotetrazole 发明人:PIERCEY DAVIN GLENN; MANSHIP TIMOTHY D; SMITH DAWSON MICHAEL 权利人:PURDUE RESEARCH FOUNDATION 摘要:This disclosure shows the ability of a readily-available oxidizer to achieve oxidation of 5-amino-1H-tetrazole (5-AT) to 5-nitrotetrazole (5-NT) in high yields in a single pot synthesis. This strategy reduces the synthesis of this important energetic material down to a single step and eliminates highly sensitive diazonium and copper salt primary explosive intermediates. The overall yield of this process is 48-53% and the resultant aqueous solution of product effectively used for the preparation of nitrotetrazole-containing primary explosive DBX-1. Unlike current methods of nitrotetrazole preparation, the novel method is entirely solution-based and prepares a final solution of sodium nitrotetrazolate, never once needing to handle energetic intermediates or products, making it a much safer method of nitrotetrazole preparation.
专利号:US-11773112-B2 优先权日:2020-12-05 标题:Synthesis of tetrazolate salts 发明人:PRADHAN BRAJA SUNDAR; SINGH SANJEEV K; MEHTA NEHA H 权利人:PRIMODIA CHEMICALS AND PHARMACEUTICALS PRIVATE LTD 摘要:The present invention relates to a novel method of synthesis of copper (I) 5-nitrotetrazolate. Particularly, for the synthesis of the copper (I) 5-nitrotetrazolate, the present invention uses a suitable salt of 5-aminotetrazole, preferably the sulfate or the nitrate salt as the starting compound. The selection of the said starting chemical not only eliminates any safety issue arising during Sandmeyer reaction conditions to affect the functional group conversion but also greatly improves the ease of executing the synthetic protocol, rendering the process safe to be adopted for commercial manufacture of the copper (I) 5-nitrotetrazolate compound.
专利号:US-9440934-B1 优先权日:2014-04-10 标 题 :Synthesis of copper(I) 5-nitrotetrazolate 发明人:MEHTA NEHA; Oyler Karl; CHENG GARTUNG; SALAN JERRY; LENAHAN SHANNON 权利人:MEHTA NEHA; Oyler Karl; CHENG GARTUNG; SALAN JERRY; LENAHAN SHANNON; US ARMY 摘要:A method of manufacture of the primary explosive material copper(I) 5-nitrotetazolate (DBX-1) by a synthesis starting with 5-aminotetrazolate (5-AT); wherein, the synthesis provides intermediates acid copper salt of 5-NT and sodium 5-nitrotetrazolate (NaNT) sodium 5-nitrotetrazolate (NaNT)—that are both, free of any 5-aminotetrazolate (5-AT) starting material—such that the subsequent production of the DBX-1 is not inhibited. Further, this method utilizes an internal filter within the reactor—to minimize handling of explosively dangerous intermediates.
专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
专利号:WO-2023230307-A1 优先权日:2022-05-27 标 题 :Methods for cobinamide synthesis 发明人:BOSS GERARD; CHAN ADRIANO 权利人:UNIV CALIFORNIA 摘要:Methods of synthesis of cobinamide compounds with improved yield and purity. Methods and compositions for treating cyanide, sulfide, sodium azide, or methane-thiol exposure in a subject.
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