CAS: 360-97-4; 4-Amino-1H-Imidazole-5-Carboxamide

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替莫唑胺置于水体系中,化学反应 2191.5H,反应生成 4-氨基-5-咪唑甲酰胺
参考文献:Temozolomide-hesperetin Drug-drug Cocrystal With Optimized Performance In Stability,Dissolution,And Tabletability
标题:Temozolomide-hesperetin Drug-drug Cocrystal With Optimized Performance In Stability,Dissolution,And Tabletability
摘要:采用液体辅助研磨,浆液转化结晶,蒸发结晶等方法成功制备了替莫唑胺和橙皮素1:1药物共晶.通过单晶和粉末x射线衍射,差示扫描量热法,热重分析,以及傅里叶变换红外光谱和核磁共振光谱对所得共晶进行了综合表征.共晶中的两个药物分子通过替莫唑胺的羰基氧和橙皮素的酚羟基之间的o-H.o氢键连接.药物-药物共晶增强了橙皮素的吸水稳定性和替莫唑胺的理化稳定性.此外,与原始药物相比,共晶体优化了替莫唑胺和橙皮素在 Ph 1.2 和 Ph 6.8 下的溶出行为.此外,还进行了可压缩性评估,与替莫唑胺相比,共晶表现出优异的可压片性.因此,药物-药物共晶有可能被开发为有效的口服药物组合制剂,克服每种母体药物的弱点.
DOI:10.1021/acs.Cgd.0C01153

专利信息

专利号:US-2006154256-A1
优先权日:2001-10-25
标 题:Method for covalently attaching nucleosides and/or nucleotides on surfaces and method for determining coupling yields in the synthesis of nucleotides
发明人：STENGELE KLAUS-PETER; KVASSIOUK EVGUENI
权利人:STENGELE KLAUS-PETER; KVASSIOUK EVGUENI
摘要:The present invention relates to a method for covalently attaching nucleosides and/or nucleotides on surfaces having reactive functional groups, where in a first step, the reactive functional groups are made to react with suitable derivatized nucleosides and/or nucleotides, and in a second step, they are converted with a protecting group reagent, so that a reaction product of the consecutive reaction interacts with electromagnetic radiation such that it can be quantitatively determined. The invention also relates to a method for determining the repetitive coupling yields in the synthesis of nucleotides where the free 3′ or 5′ hydroxy group of a selected nucleoside and/or nucleotide is converted with a compound of formula (I) n n nwhere L is a common suitable leaving group, the motif O—PX represents a phosphor amidite, a H-phosphonate a phosphonic acid ester, a phosphotriester, Yâ•?O or S, N is a nucleoside or a nucleotide derivative which subsequently reacts further with a protecting group reagent and the elimination of the leaving group (L), which is subsequently further eliminated. The quantity of the leaving group (L) eliminated in step b) is quantitatively determined in the form of its anion (L − ) by means of otical spectroscopy.

专利号:US-7737284-B2
优先权日:2001-01-18
标题 :Synthesis of temozolomide and analogs
发明人：KUO SHEN-CHUN; MAS JANET L; HOU DONALD CHEN-TUNG
权利人:SCHERING PLOUGH CORP
摘要:This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

专利号:US-6844434-B2
优先权日:2001-01-18
标题 :Synthesis of temozolomide and analogs
发明人：KUO SHEN-CHUN
权利人:SCHERING CORP
摘要:This invention relates to a novel process for the synthesis of temozolomide, an antitumor compound, and to intermediates useful in this novel process.

专利号:US-2013012706-A1
优先权日:2010-03-01
标 题 :Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines
发明人：HUMMERSONE MARC GEOFFERY; COUSIN DAVID
权利人:PHARMINOX LTD; HUMMERSONE MARC GEOFFERY; COUSIN DAVID
摘要:The present invention provides a compound of general formula (II), or a salt or solvate thereof: n n n n n n n n n n n n wherein n A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein:n -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate;n nand its use in the synthesis of temozolomide and analogues thereof.

专利号:US-11254958-B1
优先权日:2018-06-20
标 题:Metabolic engineering of E coli with thio-phosphate
发明人：FRAYNE ELIZABETH GAY
权利人:FRAYNE ELIZABETH GAY
摘要:The present invention describes the use of thio-phosphate in the metabolic engineering of E. coli . Thio-phosphate can be used to increase the metabolic flux in important synthetic pathways to enhance the production of bioproducts. The pathways impacted include the following: fatty acid synthesis, isoprenoid syntheses, Vit K2 synthesis, ribonucleotide synthesis, and the synthesis of phosphoribosyl pyrophosphate (PRPP) derivatives like 5-aminoimidazole-4-carboxamide (AICA riboside), histidine, and tryptophan. Thus, thio-phosphate can be used to assist in the production of these molecules and/or their derivatives. Enhanced production of AICA in Bacillus megaterium is also demonstrated.

专利号:US-2004203036-A1
优先权日:2001-07-09
标 题 :Multimer polynucleotide synthesis
发明人：STENGELE KLAUS-PETER; PFLEIDERER WOLFGANG
摘要:The present invention relates to a process for the preparation of polynucleotides, whereby under suitable usual conditions the free 5′-hydroxy group, whose terminal 3′-hydroxy group contains a usual protecting group, is reacted with a hydroxy group, derivatized in a previous reaction step to a phosphite amidoester, phosphpotriester or phosphonic acid ester, whereby said hydroxy group is a 3′-hydroxy function of a free or solid phase bound polynucleotide, or a solid phase bound hydroxy function. n Further the present invention relates to a kit for performing a process according to the invention, which contains at least one or more selected oligonucleotides, having a free 5′-hydroxy group and a protected 3′-hydroxy group. Further on, the present invention relates to new oligonucleotides and their use as building blocks for the synthesis of polynucleotides in the process according to the invention. n Furthermore the present invention relates to the use of the process according to the invention or the use of the kits for the preparation of poly/oligonucleotides resp. polynucleotide libraries or nucleic acid chips.