CAS: 13726-52-8; N-(4-Aminobenzoyl)-L-Glutamic Acid Diethyl Ester

上下游产品

-DL-glutaminsaeure-diaethylesterN-4-Nitro-benzoyl-DL-glutaminsaeure-diaethylester diethyl 2-aminopentanedioate 4-nitro-benzoic acid N-[4-(toluene-4-sulfonylamino)-benzoyl]-L-glutamic acid diethyl esterN-[4-(toluene-4-sulfonylamino)-benzoyl]-L-glutamic acid diethyl esterN-{4-[(2-oxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl esterN-{4-[(2-oxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl ester N-{4-[(2-thioxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl esterN-{4-[(2-thioxo-benzooxazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl ester N-{4-[(2-thioxo-benzothiazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl esterN-{4-[(2-thioxo-benzothiazol-3-ylmethyl)-amino]-benzoyl}-glutamic acid diethyl ester -benzoyl>-glutaminsaeureN-4--benzoyl-glutaminsaeure

N-(4-硝基苯甲酰)-L-谷氨酸二乙酯置于sodium Tetrahydroborate体系中,用 四氢呋喃,水 用作溶剂,化学反应 6.0H,以86%的收率获得n-(4-氨基苯(甲)酰)-L-谷氨酸二乙酯
参考文献:室温下水中可持续/可回收的fe / Ppm Pd纳米颗粒催化的安全和选择性硝基还原
标题:室温下水中可持续/可回收的fe / Ppm Pd纳米颗粒催化的安全和选择性硝基还原
摘要:由于无配体的fe / Ppm Pd纳米颗粒与含peg的设计剂表面活性剂之间具有独特的协同作用,因此在室温下水中存在nabh 4的情况下,可以轻松,选择性地还原含硝基的芳族化合物和杂芳族化合物.这项新的纳米技术涉及低催化剂负载量,高度化学选择性,并能耐受多种官能团.该过程包括整个水性介质的循环利用,它为减少有价值的含硝基化合物提供了一种通用的,对环境负责的,尤其是安全的方法.
Doi:10.1002/anie.201604026

专利信息

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-2547519-A
优先权日:
标题 :Synthesis of pteridines