[5-(Phenylthio)-1H-Benzimidazol-2-Yl]Carbamic Acid置于m-Chloroperoxybenzoic Acid,溶剂黄146体系中,用 氯仿 作为反应溶剂,化学反应生成 奥吩达唑 参考文献:Method Of Treating Helminthiasis By Parenteral Administration Of 标题:Method Of Treating Helminthiasis By Parenteral Administration Of 摘要:提供了一种治疗或抑制蠕虫病的方法,即通过经肠道给予苯并咪唑的亚氧化物衍生物,其具有结构##str1##其中r.Sup.1为较低烷基或苯基较低烷基,R.Sup.2为氢,较低烷基,卤素,较低烷氧基或硝基.还提供了用于上述方法的药物组成物.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:WO-2009094569-A2 优先权日:2008-01-25 标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
1: Son DS, Lee ES, Adunyah SE. The Antitumor Potentials of Benzimidazole Anthelmintics as Repurposing Drugs. Immune Netw. 2020 Aug 4;20(4):e29. doi: 10.4110/in.2020.20.e29. 2: Kabululu ML, Ngowi HA, Mlangwa JED, Mkupasi EM, Braae UC, Trevisan C, Colston A, Cordel C, Johansen MV. Endemicity of Taenia solium cysticercosis in pigs from Mbeya Rural and Mbozi districts, Tanzania. BMC Vet Res. 2020 Sep 3;16(1):325. doi: 10.1186/s12917-020-02543-9. 3: Bach T, Galbiati S, Kennedy JK, Deye G, Nomicos EYH, Codd EE, Garcia HH, Horton J, Gilman RH, Gonzalez AE, Winokur P, An G. Pharmacokinetics, Safety, and Tolerability of Oxfendazole in Healthy Adults in an Open Label Phase 1 Multiple Ascending Dose and Food Effect Study. Antimicrob Agents Chemother. 2020 Aug
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参考文献:10.1186/2046-0481-64-4 摘要:Patten T, Good B, Hanrahan JP, Mulcahy G, de Waal T. Gastrointestinal nematode control practices on lowland sheep farms in Ireland with reference to selection for anthelmintic resistance. Irish Veterinary Journal. 2011 Mar 31;64(1):4. doi: 10.1186/2046-0481-64-4.