合成目标产物 N,N-Dimethylglycine Hydrochloride 主要起始原料 Dimethylamine And Chloroacetic Acid
(文献来源)合成步骤主要原料 Dimethylamine 和 Chloroacetic Acid
N,N-二甲基甘氨酸置于盐酸体系中,用 乙醇,水,丙酮 用作溶剂,化学反应生成N,N-二甲基甘氨酸盐酸盐 参考文献:Novel Tween® 20 Derivatives Enable The Formation Of Efficient Ph-Sensitive Drug Delivery Vehicles For Human Hepatoblastoma 标题:Novel Tween® 20 Derivatives Enable The Formation Of Efficient Ph-Sensitive Drug Delivery Vehicles For Human Hepatoblastoma 摘要:We Describe The Synthesis,The Physicochemical Characterization And The Biological Evaluation Of Three Novel Ph-Sensitive Systems Prepared Derivatizing Polysorbate 20 (Tween (R) 20) With Glycine,N-Methylglycine And N,N-Dimethyl-Glycine (Tw20-Gly,Tw20-Mmg And Tw20-Dmg). These Derivatives Form Ph-Sensitive Vesicles And Translocate Small Molecules Into Cells. The Reported Systems Are Efficient Drug Delivery Systems For Human Hepatoblastoma Cells. (C) 2010 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2010.04.010
专利号:US-6166031-A 优先权日:1987-10-19 标 题:Substituted tetralins, chromans and related compounds in the treatment of asthma 发明人:EGGLER JAMES F; MARFAT ANTHONY; MELVIN JR LAWRENCE S 权利人:PFIZER 摘要:Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals; pharmaceutical compositions comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
专利号:EP-0309300-B1 优先权日:1987-09-21 标题:Process for the preparation of dimethylglycylgluconic-acid salts 摘要:A new process for the synthesis of pangamic acid salts (sometimes also referred to as vitamin B15 and more accurately called dimethylglycyl gluconates). This process consists in the esterification of gluconic acid or of calcium or magnesium gluconate with a dimethylglycine hydrochloride in aqueous medium in the presence of phosphoric acid or of sulphuric acid at a temperature varying between 30 DEG and 70 DEG C; then in the concentration of the esterification product, followed by removal of the inorganic acids by reaction with a water-insoluble amine of high molecular weight. The pangamic acid obtained is then converted into one of its salts by reaction with a carbonate such as, for example, calcium carbonate or magnesium carbonate. The pangamates are useful in medicine for combating various forms of arteriosclerosis.
专利号:US-9051289-B2 优先权日:2013-09-26 标 题 :Process and intermediates for preparing GPR40 agonists 发明人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN 权利人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I n nwherein R S denotes F or CF 3 , R a denotes H or C 1-4 -alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
专利号:US-5998451-A 优先权日:1987-10-19 标 题 :Substituted tetralins, chromans and related compounds in the treatment and related compounds in the treatment of asthma, arthritis and related diseases 发明人:EGGLER JAMES F; MARFAT ANTHONY; MELVIN JR LAWRENCE S 权利人:PFIZER 摘要:Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
专利号:US-5298512-A 优先权日:1989-04-07 标 题:Substituted chromans and their use in the treatment of asthma, arthritis and related diseases 发明人:EGGLER JAMES F; MARFAT ANTHONY; MASAMUNE HIROKO; MELVIN JR LAWRENCE S 权利人:PFIZER 摘要:Substituted chromans which by inhibiting 5-lipoxygenase enzyme are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction, stroke and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
专利号:WO-2024081885-A1 优先权日:2022-10-13 标 题 :Method for inhibiting clostridioides difficile spore germination 发明人:QIAN YUANYUAN; CHANG MAYLAND; MOBASHERY SHAHRIAR 权利人:UNIV NOTRE DAME DU LAC 摘要:Oxadiazole antibiotics that exhibit bactericidal activity against C. difficile vegetative cells. We screened a library of 75 oxadiazoles against C. difficile ATCC 43255. The findings from this collection served as the basis for the syntheses of an additional 58 analogs, which were tested against the same strain. We discovered a potent (MIC 50 = 0.5 µg/mL, MIC 90 = 1 µg/mL for 101 C. difficile strains) and narrow-spectrum oxadiazole (3-(4-(cyclopentyloxy)phenyl)-5-(4-nitro-1 H -imidazol-2-yl)-1,2,4-oxadiazole; compound 57) that is not active against common gut bacteria or other tested organisms, but is selectively bactericidal against C. difficile and targets cell-wall synthesis. Other similarly effective oxadiazole antibiotics of formula I and II are described herein, several of which inhibit or prevent C. difficile spore germination.