专利号:US-8686157-B2 优先权日:2003-02-10 标题:Processes for the facile synthesis of diaryl amines and analogues thereof 发明人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN 权利人:SNOONIAN JOHN R; OLIVER-SHAFFER PATRICIA ANN; VERTEX PHARMA 摘要:The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.
专利号:US-3933830-A 优先权日:1974-09-10 标 题 :Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines 发明人:BARTH WAYNE E; KUHLA DONALD E 权利人:PFIZER 摘要:Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms. n Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art. n The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
专利号:US-9481649-B2 优先权日:2009-08-24 标题 :Synthesis of a neurostimulative piperazine 发明人:VENKATRAMAN SRIPATHY; MAHMOOD SYED; MOBELE BINGIDIMI I; LAPINA OLGA; VERCOE KELLIE; LI YING; SALSBURY JONATHAN; MCLAWS MARK 权利人:NEURALSTEM INC 摘要:The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.
专利号:WO-2016118586-A1 优先权日:2015-01-20 标 题 :Lowcost, high yield synthesis of nevirapine 发明人:AHMAD SAEED; GUPTON FRANK; VERGHESES JENSON; MCQUADE TYLER 权利人:UNIV VIRGINIA COMMONWEALTH 摘要:Improved methods of producing the HIV drug substance, nevirapine are provided. The methods employ a cost effective and high yield synthetic methods for preparing the nevirapine building block 2-chloro-3-amino-4-picoline (CAPIC) and 2-cyclopropyl amino nicotinate (Me-CAN), and improvements in other steps of nevirapine synthesis.
专利号:US-2023202980-A1 优先权日:2019-08-30 标题:N-(2-Aminophenyl)-Prop-2-Enamide Derivatives, and Uses Thereof in the Treatment of Cancer 发明人:RADHAKRISHNAN SRIDHAR; TENEN DANIEL G; LIU BEE HUI; VU LE KIM ANH; GO MEI LIN; CHAI LI; GAO CHONG; KAMAL AHMED; SUNKARI SATISH; AYINAMPUDI VENKATA SUBBARAO; SYED RIYAZ; LIU MIAO 权利人:NAT UNIV SINGAPORE; THE BRIGHAM AND WOMEN’S HOSPITAL INC; INDIAN INSTITUTE OF CHEMICAL TECH 摘要:Provided herein are N-(2-aminophenyl)-prop-2-enamide derivatives, such as those of Formula (I), methods for the synthesis thereof, and uses thereof in the treatment of cancer, such as SALL4-expressing cancer, in a cell or subject in need thereof.
专利号:US-2025178999-A1 优先权日:2022-03-18 标 题:One step synthesis of 1-tetralone compounds and uses thereof in the preparation of (+)-tetralone abscisic acid (aba) 发明人:DIDDI NAVEEN; ABRAMS SUZANNE ROBERTA; LAI LEON 权利人:UNIV SASKATCHEWAN 摘要:The present application is related to a process for preparing 1-tetralone compounds such as compounds of Formula I by reacting a,; 3-unsaturated cyclic ketones that comprise two available hydrogens on the y carbon to the carbonyl with acrolein derivatives with heating in the presence of a suitable organic acid, a suitable organic amine base and suitable inert solvent. For example, the 1-tetralone compound is a tetralone derivative of abscisic acid (ABA).
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