📜二氯乙酸置于盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 二氯乙酸酐 参考文献:Ctc-[pt(Nh3)2(Cinnamate)(Valproate)Cl2] Is A Highly Potent And Low-Toxic Triple Action Anticancer Prodrug 标题:Ctc-[pt(Nh3)2(Cinnamate)(Valproate)Cl2] Is A Highly Potent And Low-Toxic Triple Action Anticancer Prodrug 摘要:Cin-Pt(Iv)-Val前药通过一种协同机制发挥比顺铂更有效的体外和体内抗肿瘤活性,该机制涉及dna损伤以及对hdac和mmp-2和9活性的抑制. DOI:10.1039/d1Dt01421H
专利号:US-4756739-A 优先权日:1985-12-21 标题 :Pyridine derivatives and the N-oxides thereof, and the use thereof as intermediates for the synthesis of plant protecting agents 发明人:FUSS ANDREAS; KOCH VOLKER 权利人:HOECHST AG 摘要:The compounds of the formula I (I) in which A denotes N or N->O, Z denotes O or NH, R denotes H, (halo)alkyl, (halo)alkenyl, (halo)alkynyl or alkoxycarbonyl, R1 denotes hydrogen, halogen, amino, -NHOH, hydroxyl, (substituted) phenylazo or a radical of the formulae Y=C=N-, Y1Y2C=N-, Y3NH- or K denotes 0 or 1, and m and n, independently of one another, denote a number from 1 to 4, with the proviso that, when Z-R denotes OH or NH2, (R1)n denotes at least one radical of the formula or represents two radicals, in the 5 or 6 position of the heterocyclic ring, which, in the 5 position, denote halogen and, in the 6 position, denote a radical of the group comprising halogen, amino, hydroxyl or phenylazo, which may be substituted as specified above, are valuable intermediates in the synthesis of plant protection agents.
专利号:US-4255594-A 优先权日:1979-09-18 标题 :Hydrogenation of halogen-containing carboxylic anhydrides 发明人:NOVOTNY MIROSLAV 权利人:ALLIED CHEM 摘要:A process is described for the heterogeneous hydrogenation of haloalkyl, halocycloalkyl or haloaryl carboxylic anhydrides to the corresponding primary alcohols. In the haloalkyl or halocycloalkyl carboxylic anhydrides at least one halogen is in the alpha-position relative to the carboxylic anhydride grouping. The hydrogenation can be carried out in the liquid or vapor phase in the presence of a supported or unsupported catalyst comprising a member of the group consisting of rhodium, iridium, metal oxides thereof, or mixtures thereof. In the liquid phase, the hydrogenation can be carried out batchwise under mild conditions of temperature and pressure, preferably at about 50°-150° C. and about 5-15 atmospheres, in an atmosphere containing hydrogen gas. A preferred embodiment is the hydrogenation of trifluoroacetic anhydride in the liquid phase to 2,2,2-trifluoroethanol, said alcohol being useful as an intermediate in the synthesis of the anesthetic, isoflurane, CF 3 CHClOCHF 2 .
专利号:US-7884128-B2 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D 发明人:KANADA REGINA MIKIE; ITO DAISUKE; SAKAI TAKASHI; ASAI NAOKI; KOTAKE YOSHIHIKO; NIIJIMA JUN 权利人:EISAI R&D MAN CO LTD 摘要:Process for producing compound of Formula: n nwherein P 2 , P 3 and R 2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7):n n nwherein P 3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8):n n nwherein P 2 means a protecting group for hydroxy group; and R 2 means a phenyl group which may be substituted, in the presence of a base.
专利号:US-9688657-B2 优先权日:2013-03-25 标题:Synthesis of dabigatran 发明人:PATKAR LAXMIKANT NARHARI; MONDKAR HARISH KASHINATH; AROTE NITIN DNYANESHWAR; PATIL SACHIN SHIVAJI; JADHAV TANAJI SHAMRAO; HAGAVANE NITIN NIVRUTTI; BHOPALKAR RAJESH GANPAT 权利人:USV PRIVATE LTD 摘要:The present invention relates to a process for preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof. The present invention relates to novel compounds, in particular Ethyl-3-{[(2-formyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl) amino}propanoate and Ethyl-3-{[(2-dichloromethyl-1-methyl-1H-benzimidazole-5-yl)carbonyl]-(2-pyridinyl)amino}propanoate and process for preparation thereof. The present invention further relates to the use of these novel compounds in the preparation of Dabigatran etexilate or pharmaceutically acceptable salt thereof.
专利号:US-9376400-B2 优先权日:2005-06-08 标 题:Process for the synthesis of triazoles 发明人:CHEN SHILI; LOU RONGLIANG; WU YUSHENG; ZHOU JIACHENG; HANSELMANN ROGER 权利人:MELINTA THERAPEUTICS INC 摘要:The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
专利号:US-7301049-B2 优先权日:2001-06-21 标 题:Photolabile esters and their uses 发明人:SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN 权利人:CANCER RES INST 摘要:Compounds which are capable of generating acid on photolysis are disclosed, and the uses of these compounds, especially for deprotecting the termini of nucleic acid molecules or peptides during synthesis of arrays. The compounds described herein may be employed in the detritylation of 5′-O-dimethoxytrityl (DMT) protected nucleotides by photolysing the compounds to generate an acid capable of removing the DMT group allowing oligonucleotide arrays to be synthesised using readily available 5′-O-DMT-nucleoside-3′-O-phosphoramidite monomers conventionally used in solid phase nucleic acid synthesis. A method of avoiding the effects of stray light in projection lithography techniques is also disclosed.
[参考文献]: Ping Cai, Et Al. Autoimmune Response In Mrl+/+ Mice Following Treatment With Dichloroacetyl Chloride Or Dichloroacetic Anhydride. Toxicol Appl Pharmacol. 2006 Oct 15;216(2):248-55.
合成参考文献
参考文献:10.1016/j.taap.2006.05.010 摘要:Cai P, König R, Khan MF, Qiu S, Kaphalia BS, Ansari GA. Autoimmune response in MRL+/+ mice following treatment with dichloroacetyl chloride or dichloroacetic anhydride. Toxicol Appl Pharmacol. 2006 Oct 15;216(2):248–55. doi: 10.1016/j.taap.2006.05.010. 摘要:AMA Archives of Industrial Hygiene and Occupational Medicine., 4(119), 1951