2-吡啶甲酸置于氯化亚砜,Sodium Hydroxide体系中,化学反应 97.0H,反应生成 4-氯-2-吡啶甲酸 参考文献:Dual-Action Inhibitors Of Hif Prolyl Hydroxylases That Induce Binding Of A Second Iron Ion 标题:Dual-Action Inhibitors Of Hif Prolyl Hydroxylases That Induce Binding Of A Second Iron Ion 摘要:翻译结果: 对缺氧诱导因子(hif)脯氨酰羟化酶(phd或egln酶)的抑制在治疗贫血和缺血相关疾病方面备受关注.大多数phd抑制剂通过结合单个亚铁离子并与2-氧代戊二酸(2Og)共底物竞争结合phd活性位点来发挥作用.非特异性铁螯合剂也能在体外和细胞内抑制phd.我们报告了双作用phd抑制剂的鉴定,这些抑制剂不仅与活性位点的铁结合,还能诱导在活性位点上结合第二个铁离子.通过对小分子铁络合物的分析并在非变性蛋白质谱法中评估phd2.铁.抑制剂的比例后,鉴定出某些二酰基联氨为诱导第二个铁离子结合的phd2抑制剂.有些化合物被证明能抑制人类肝癌和肾癌细胞系中的hif羟化酶. DOI:10.1039/c2Ob26648B
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-2025115629-A1 优先权日:2021-03-18 标 题 :Chiral synthons for the synthesis of chiral phosphorothioates 发明人:ZHANG YONGDA; WU LINGLIN 权利人:BOEHRINGER INGELHEIM INT 摘要:This invention relates to compounds of Formula (I) useful as synthons for a general synthetic method for making chiral phosphorothioates, to their preparation and to their use in a robust large scale process for making P-chiral phosphorothioates.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:EP-3686190-A1 优先权日:2013-07-11 标 题 :Synthesis of therapeutically active compounds
专利号:WO-2022194924-A1 优先权日:2021-03-18 标 题:Chiral synthons for the synthesis of chiral phosphorothioates
专利号:US-12304912-B2 优先权日:2020-07-28 标 题 :Fused bicyclic RAF inhibitors and methods for use thereof 发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA 权利人:JAZZ PHARMACEUTICALS IRELAND LTD 摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 160. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 291. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 269. 摘要:A. N. Kost, P. B. Terentev, L. A. Golovleva and A. A. Stolyarchuk, Khim.-Farm. Zh. 1, 3 (1967); CA 68, 29556a.