CAS: 364-62-5; Metoclopramide

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CAS号7206-70-4 4-氨基-5-氯-2-甲氧基苯甲酸 | CAS号100-36-7 N,N-二乙基乙二胺 | CAS号54769-22-1 1-methanesulfon... | CAS号201230-82-2 carbon monoxide | CAS号27492-84-8 2-甲氧基-4-氨基苯甲酸甲酯 | CAS号2401-24-3 2-氯-5-甲氧基苯胺 | CAS号150007-96-8 4-amino-5-chlor... | CAS号4093-29-2 胃复安甲基物 | CAS号38059-78-8 O-去甲基甲氧氯普胺盐酸盐 | CAS号171367-22-9 甲氧氯普安N氧化物 | CAS号27260-19-1 N-Desethyl Meto... | CAS号102670-59-7 4-amino-5-chlor... | CAS号65569-29-1 氯沙必利 | CAS号38339-95-6 4-amino-5-chlor...

5-Chloro-N-[2-(Diethylamino)Ethyl]-4-(Dimethylaminomethylideneamino)-2-Methoxybenzamide置于乙二胺,水体系中,用 乙醇 用作溶剂,化学反应 10.0H,以2.32 G的收率获得甲氧氯普胺
参考文献:The Use Of Formamidine Protection For The Derivatization Of Aminobenzoic Acids
标题:The Use Of Formamidine Protection For The Derivatization Of Aminobenzoic Acids
摘要:N,N-Dimethylformamidine And Novel N,N-Diisopropylformamidine Protecting Groups Were Used To Carry Out A One-Pot Conversion Of Aminobenzoic Acids Into The Corresponding Amides. General Conditions For An In Situ Transformation Of Aminobenzoic Acids And Their Heterocyclic Analogues Into The Corresponding Formamidine-Protected Acid Chlorides Were Developed. These Chlorides Were Used In Reactions With Amines,Including Poorly Reactive Anilines. The Protected Amides Were Then Smoothly Deprotected By Heating With Ethylenediamine Derivatives,Resulting In A General Procedure For The One-Pot Transformation Of Aminobenzoic Acids Into Their Amides. Our One-Pot Procedure Was Successfully Applied To The Preparation Of Several Compounds Of Pharmaceutical Interest.
Doi:10.1021/jo8017186

专利信息

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:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2008267981-A1
优先权日:2004-06-30
标题:Compositions and Methods for Delivery of Antitumor Agents
发明人：JANDA KIM D; WIRSCHING PETER; BOGER DALE L
权利人:SCRIPPS RESEARCH INST
摘要:Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.