合成目标产物 1-Chloroethyl Chloroformate 主要起始原料 Acetaldehyde And Diphosgene
(文献来源)合成步骤主要原料 Acetaldehyde 和 Diphosgene
氯甲酸乙酯置于过氧化苯甲酰体系中,用 磺酰氯 作为反应溶剂,化学反应生成 1-氯乙基氯甲酸酯 参考文献:Prodrugs Of Imidazole Carboxylic Acids As Angiotensin Ii Receptor 标题:Prodrugs Of Imidazole Carboxylic Acids As Angiotensin Ii Receptor 摘要:咪唑羧酸的前药是aii拮抗剂,对治疗高血压有用,公开了这些前药的药物组合物以及使用这些前药治疗高血压的方法.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
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-5220016-A 优先权日:1991-07-29 标 题:Synthesis of navelbine analogs 发明人:MAGNUS PHILIP D; THURSTON LEE S 权利人:UNIV TEXAS 摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
专利号:US-4592874-A 优先权日:1980-05-14 标 题:Process for the synthesis of alpha-chlorinated chloroformates 发明人:CAGNON GUY C; PITEAU MARC D; SENET JEAN-PIERRE G; OLOFSON ROY A; MARTZ JONATHAN T 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:Process for the synthesis of alpha -chlorinated chloroformates, and new alpha -chlorinated chloroformates. The invention relates to a new process for the manufacture of alpha -chlorinated chloroformates and, to new alpha -chlorinated chloroformates as new industrial products. The process according to the invention consists of a synthesis, by catalytic phosgenation, of alpha -chlorinated chloroformates of the formula: in which: R represents a substituted or unsubstituted hydrocarbon radical and m represents an integer superior or equal to one, this synthesis consisting in reacting phosgene with the aldehyde R-CHO)m, in the presence of a catalyst which is an organic or inorganic substance which is capable in a medium containing an aldehyde of the formula R-CHO)m, phosgene and, possibly, a solvent, of generating a pair of ions one of which is an halogenide anion and the other is a cation which is sufficiently separated from said halogenide anion so as to give to the latter a nucleophilic power enabling it to react with the function(s) aldehyde of the molecule R-CHO)m.
专利号:US-7423169-B2 优先权日:2001-06-11 标 题:Methods for synthesis of acyloxyalkyl derivatives of GABA analogs 发明人:RAILLARD STEPHEN P; ZHOU CINDY X; YAO FENMEI; MANTHATI SURESH KUMAR; XIANG JIA-NING; GALLOP MARK A 权利人:XENOPORT INC 摘要:The synthesis of 1-(acyloxy)-alkyl carbamates of GABA analogs from 1-haloalkyl carbamates of GABA analogs are described. Also described are new 1-haloalkyl carbamates of GABA analogs.
专利号:WO-2012088402-A1 优先权日:2010-12-22 标题 :Synthesis of conolidine and discovery of a potent non-opioid analgesic for pain 发明人:BOHN LAURA M; MICALIZIO GLENN C 权利人:SCRIPPS RESEARCH INST; BOHN LAURA M; MICALIZIO GLENN C 摘要:The first de novo synthetic pathway to the exceptionally rare C5-nor stemmadenine natural product, conolidine, and the first asymmetric synthesis of any member of this natural product class arc described. C5-nor stemmadenine compositions are also described. These compounds, for example,(+/- )-,(+)- and (-)-conolidine are potent and efficacious non-opioid analgesics in tonic and persistent pain.
参考标题:Alkyl 1-Chloroalkyl Carbonates: Reagents For The Synthesis Of Carbamates And Protection Of Amino Groups 作者:Gérard Barcelo,Jean-Pierre Senet,Gérard Sennyey,Jean Bensoam,Albert Loffet 摘要:The Synthesis Of 1-Chloroalkyl Carbonates And Their Reaction With Various Type Of Amines Are Described. This Reaction Is Useful For The Synthesis Of Carbamate Pesticides And For The Protection Of Various Amino Groups, Including Amino Acids.
合成参考文献
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 347. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).