CAS: 437-74-1; 7-(2-Hydroxy-3-((2-Hydroxyethyl)(Methyl)Amino)Propyl)-1,3-Dimethyl-1H-Purine-2,6(3H,7H)-Dione Nicotinate

上下游产品

7-{2-hydroxy-3-[(2-hydroxyethyl)(methyl)amino]propyl}-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione nicotinic acid theophylline 1,3-dimethyl-7-(oxiran-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione

茶碱置于potassium Carbonate体系中,用 N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 73.5H,反应生成 烟酸占替诺
参考文献:对映体富集的二丙茶碱和烟酸黄嘌呤醇的化学酶法合成
标题:对映体富集的二丙茶碱和烟酸黄嘌呤醇的化学酶法合成
摘要:首次报道了一种针对富含对映体的活性药物成分 (Api)--diprophylline 和 Xanthinol Nicotinate 的简明化学酶途径.的决定性步骤是外消旋氯醇合成子乙酸盐,即1-氯-3-(1,3-二甲基-2,6-二氧代-1,2,3,6-四氢-7-的对映选择性脂肪酶介导的甲醇分解ħ-Purin-7-yl)Propan-2-Yl醋酸盐,在动力学控制条件下进行,制备规模为 500 Mg.使用来自南极念珠菌的b 型脂肪酶进行对映异构体拆分,在反应对映选择性方面获得了最佳结果 (E = 14)固定在丙烯酸树脂(cal-B,Novozym 435)上,悬浮在同相乙腈-甲醇混合物中.精心设计的生物催化系统提供了关键的氯醇中间体(71% Ee 和 38% 产率),然后将其顺利转化为富含对映体的活性剂:(R)-(-)-Diprophylline (57% Ee) 和 (S)-(
DOI:10.1016/j.Bioorg.2020.104448

专利信息

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-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-2006097348-A1
优先权日:2005-03-15
标 题:Use of agents such as nonpolymeric nitric oxide donors for making the lips full again and/or colouring the lips
发明人：CALS-GRIERSON MARIE-MADELEINE
权利人:OREAL; CALS-GRIERSON MARIE-MADELEINE
摘要:The invention relates in particular to the cosmetic use (i) of at least one agent for promoting the production of NO in and/or on the lips, chosen from nitric oxide NO donors or precursors; nonpolymeric NO releasers; and NO synthase synthesis and/or activity stimulators; or (ii) of other agents for promoting microcirculation in the skin, chosen from potassium channel openers; calcium channel blockers; phosphodiesterase inhibitors; flavonoids; vasodilator peptides that are not NO donors; temperature modulators; agents for promoting the stimulation and/or maintenance of angiogenesis; agents for promoting the stimulation of endothelial cell proliferation; agents for promoting endothelial cell migration; and mixtures thereof, in a makeup and/or care composition for the lips, as an agent for naturally making the lips full again and/or naturally coloring the lips. It also relates to specific care and/or makeup compositions for the lips containing said agent, and also to a cosmetic process aimed at making the lips naturally full and/or colored, using said compositions .

专利号:CN-105658622-A
优先权日:2013-10-24
标 题:Process for the synthesis of mercaptans by the addition of hydrogen sulfide to alkenes

专利号:US-2005070715-A1
优先权日:2003-07-15
标 题:Methods for synthesis of acyloxyalkyl compounds

专利号:CN-113061135-A
优先权日:2021-03-16
标题:A kind of method for microchannel continuous synthesis of niacin zantino