CAS: 1004-74-6; 2,4,5,6-Tetraaminopyrimidine

相似化合物

5392-28-9 118-70-7 13754-19-3

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CAS号1006-23-1 2,4,6-三氨基-5-亚硝基嘧啶 | CAS号24867-36-5 5-硝基-2,4,6-三氨基嘧啶 | CAS号7647-01-0 盐酸 | CAS号1425-63-4 双肼酞嗪 | CAS号945-24-4 2,4-二氨基-6-羟甲基蝶啶 | CAS号24867-33-2 Formamide,N-(2,... | CAS号28951-77-1 Acetamide,2-hyd... | CAS号26216-55-7 9H-Purine-2,6-d... | CAS号73978-41-3 2,4-二氨基-6-羟甲基蝶啶 盐酸盐 | CAS号677297-51-7 3,3'-(2,4-二氨基-6... | CAS号33047-42-6 4-[2-(2,4-diami... | CAS号19741-14-1 4-氨基-4-脱氧-10-甲基蝶酸 | CAS号1127-93-1 2,4-Pteridinediamine

5-亚硝基-2,4,6-三氨基嘧啶置于sodium Sulfate体系中,用 甲醇,水 用作溶剂,化学反应生成2,4,5,6-四氨基嘧啶
参考文献:咪唑并吡啶-和嘌呤-硫代乙酰胺衍生物:核苷酸焦磷酸酶/磷酸二酯酶1(npp1)的强抑制剂.
标题:咪唑并吡啶-和嘌呤-硫代乙酰胺衍生物:核苷酸焦磷酸酶/磷酸二酯酶1(npp1)的强抑制剂.
摘要:核苷酸焦磷酸酶/磷酸二酯酶1(npp1)属于胞外核苷酸酶家族,可控制细胞外核苷酸,核苷和(di)磷酸盐的水平.为了研究具有药物样特性的npp1强效和选择性抑制剂的(病理)生理作用.因此,使用比色测定法以对硝基苯基5'-胸苷单磷酸酯(p-Nph-5'-Tmp)作为人工底物,筛选化合物库中的npp1抑制剂.这导致发现2-(3 H-咪唑并[4,5-B ]吡啶-2-基硫基)-N-(3,4-二甲氧基苯基)乙酰胺(5A)为具有k I的命中化合物.值为217 Nm.随后的结构-活性关系研究导致了嘌呤和咪唑并[4,5-B ]吡啶类似物的开发,用p-Nph-5'-进行测定具有高抑制力(k I值分别为5.00 Nm和29.6 Nm).以tmp为底物.出乎意料的是,与atp作为底物相比,测试时这些化合物的效力明显较低,K I值在低微摩尔范围内.对原型抑制剂的抑制机理进行了研究,发现该抑制剂与两种底物都具有竞争性.
Doi:10.1021/jm501434Y

专利信息

专利号:US-4306064-A
优先权日:1980-03-25
标 题:Synthesis of 2,4-diamino-6-hydroxymethylpteridine
发明人：ELLARD JAMES A; SATANEK JR JOSEPH
权利人:ELLARD JAMES A; SATANEK JR JOSEPH
摘要:In a method of preparing methotrexate from a coupling of 2,4-bis(triphenylphosphazino)-6-bromomethylpteridine hydrobromide with ethyl N-(p-methylamino)-benzoyl-L-glutamate to produce the phosphazino derivative of methotrexate ester and subsequently hydrolyzing the phosphazino and ester groups to produce the free methotrexate, the pteridine synthesis step wherein molecular oxygen is substituted for reaction air and the pH throughout the pteridine synthesis is regulated to between 2.5 and 5.4, the preferred pH being about 3.0 and producing from tetraaminopyrimidine and dihydroxyacetone the isomer 2,4-diamino-6-hydroxymethylpteridine over 2,4-diamino-7-hydroxymethylpteridine in a ratio of about 20:1. Exemplary of other situations involving pteridine where the molecular oxygen may be substituted for reaction air are: in the production of folic acid, tetrahydrofolic acid, etc.

专利号:WO-2013164856-A1
优先权日:2012-05-04
标题 :A process for preparing intermediates of 10-propargyl-10-deazaaminopterin (pralatrexate) synthesis and the intermediates thereof
发明人：ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD
权利人:AVRA LAB PRIVATE LTD; ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD
摘要:A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaaminopterin (Pralatrexate) is obtained by peptide formation and ester hydrolysis of the intermediate compound 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid by methods known in the art.

专利号:US-4167633-A
优先权日:1977-07-20
标题 :Preparation of 2,4,5,6-tetraaminopyrimidine from 2,4,6-triaminopyrimidine
发明人：MORROW THOMAS J
权利人:US HEALTH EDUCATION & WELFARE
摘要:An improved process for the production of ##STR1## FROM ##STR2## WHICH PRODUCES BUT DOES NOT ISOLATE AN INTERMEDIATE ##STR3## WHICH COMPOUND IS RETAINED IN SITU AND MINIMIZES THE COMPLEX POLYMER FORM OF A THREE-DIMENSIONAL NETWORK OF AZO LINKAGES FORMED BY THE NITROSO AND AMINO GROUPS. These groups, as they appear in the nitroso intermediate, have carcinogenic possibilities. It has been found that the nitroso compound will precipitate as a stirrable slurry if the temperature parameter is kept low at about 0°-20° C. A preferred route for the production of the nitroso compound from the triamino starting material utilizes as reactants 1.0-1.05 moles of sodium nitrite and 1.5 moles of HOAc in water (HCl may be substituted for HOAc). In the second state of this sequential reaction, the reduction of nitroso is carried out by a reducing agent and one preferred agent is sodium dithionite. Catalytic agents such as Raney nickel and hydrazine or nickel salts, e.g., nickel chloride, and sodium borohydride may also be used. The present process is an improvement in part of the technique of Piper and Montgomery, J. Het. Chem., 11:279 (1974), which process is designed specially to produce the antifolate methotrexate as an end product and is an improvement of the method of application Ser. No. 742,450 of Ellard filed Nov. 17, 1976, entitled 'Improved Synthesis of Methotrexate', U.S. Pat. No. 4,080,825.

专利号:US-4080325-A
优先权日:1976-11-17
标 题 :Synthesis of methotrexate
发明人：ELLARD JAMES A
权利人:US HEALTH EDUCATION & WELFARE
摘要:The present invention consists of three process improvements in the so-called multi-step Piper-Montgomery process designed especially to produce the antifolate methotrexate which is closely related to both aminopterin and folic acid. 2,4,5,6-tetraaminopyrimidine sulfite is one starting material and is usually produced in the form of the bisulfite in an acetate buffer. The present modification positively produces the hydrochloride from the bisulfite and eliminates the acetate buffer utilized in prior art processes. Subsequently, a pteridine ring is formed from the pyrimidine hydrochloride using dihydroxyacetone at pH 5.5±0.2 to form the second ring. This strict pH control together with the use of hydrochloride salt minus the acetate buffer assists in preferentially favoring the formation of 2,4-diamino-6-hydroxymethylpteridine. Subsequently the 6-hydroxy-methyl compound is converted to the hydrobromide acid salt and reacted with three moles of a triphenyl dibromophosphorane and phosphazine protecting groups are formed on the amine groups of the pteridine ring as the 6-hydroxymethyl group is transformed to 6-bromomethyl, a key intermediate. The present process leaves the protecting phosphazine groups on the primary amino groups to discourage side reactions during subsequent alkylation of the other major reactant, ethyl N-(p-methylaminobenzoyl)-L-glutamate. Furthermore, ethyl N-(p-methylaminobenzoyl)-L-glutamate, the other reactant, is uniquely produced for the present multi-step reaction by a process proceeding from ethyl N-(p-trifluoromethylaminobenzoyl)-L-glutamate by utilizing an alkali metal hydroxide in a lower (C 1 -C 6 ) alkanol wherein the protective trifluoroacetyl groups are removed. This step uses a special mixture preferably of an alkali metal hydroxide in ethanol and optimally 1 equivalent of KOH in 20% ethanol at or below ambient temperature where the mixture is added slowly to keep the reaction pH below 9. The combination of these improvements results in the increase of an overall yield of methotrexate from the named starting reactants from about 25% to approximately 40-50%.

专利号:US-2007243147-A1
优先权日:2004-07-24
标 题:Skin and/or Hair Composition Containing Compounds for Increasing The Tanning of Skin
发明人：WOLBER RAINER; TOM DIECK KAREN; SCHERNER CATHRIN; SCHLENZ KATHRIN; KRUSE INGE
权利人:BEIERSDORF AG
摘要:The invention relates to agents that are to be applied to the skin or hair and contain compounds for intensifying tanning of the skin and increasing melanin synthesis in skin or hair. The invention particularly relates to cosmetic or dermatological preparations. Using said preparations results in inducing and intensifying the tanning mechanisms of the skin, intensifying the hair color, and thus also increasing intrinsic protection of the skin or hair.

专利号:US-9943809-B2
优先权日:2014-02-27
标题 :Solvent resistant thin film composite membrane and its preparation
发明人：DOM ELKE; HERMANS SANNE; KOECKELBERGHS GUY; VANKELECOM IVO
权利人:KATHOLIEKE UNIV LEUVEN KU LEUVEN RESEARCH & DEVELOPMENT; UNIV LEUVEN KATH
摘要:The present invention relates to improved methods for synthesis of thin film composite membranes by interfacial polymerization. More in particular, the method of the present invention comprises the impregnation of an ultrafiltration porous support membrane with an aqueous solution containing a polyfunctional nucleophilic monomer, and contacting the impregnated support membrane with a second largely water-immiscible solvent containing a polyfunctional epoxide monomer.