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三光气,正己醇置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 氯甲酸正己酯
参考文献:对乙酰氨基酚,茶碱和 6-巯基嘌呤的 N-烷基-N-烷氧基羰基氨基甲基前药衍生物的实用合成
标题:对乙酰氨基酚,茶碱和 6-巯基嘌呤的 N-烷基-N-烷氧基羰基氨基甲基前药衍生物的实用合成
摘要:摘要 我们报告了对乙酰氨基酚,茶碱和 6-巯基嘌呤的 N-烷基-N-烷氧基羰基氨基甲基 (Nanaocam) 前药的新合成,通过用 N-烷基-N-烷氧基羰基氨基甲基氯化物对相应的药物分子进行烷基化,收率非常好.大多数烷基化剂是通过 N-烷基氨基甲酸烷基酯的氯甲基化有效合成的,而 N-烷基氨基甲酸烷基酯又由烷基胺和氯甲酸烷基酯制成.在没有氯甲酸烷基酯的情况下,N-烷基氨基甲酸烷基酯的合成是通过将醇转化为氯甲酸酯或活化酰化剂如酰基咪唑或对硝基苯基碳酸酯,然后与烷基反应来完成的.胺类.
DOI:10.1080/00397910600943501

专利信息

专利号:US-7138526-B1
优先权日:1999-06-15
标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
发明人：HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M
权利人:AVENTIS PHARMA INC
摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries

专利号:US-9533971-B2
优先权日:2012-10-29
标 题 :Process for the synthesis of dabigatran and its intermediates
发明人：PULLAGURLA MANIK REDDY; RANGISETTY JAGADEESH BABU; NANDAKUMAR MECHERIL VALSAN
权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD; BIOPHORE INDIA PHARMACEUTICALS PVT LTD
摘要:The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.

专利号:US-10077251-B2
优先权日:2012-10-29
标题:Process for the synthesis of Dabigatran Etexilate and its intermediates
发明人：PULLAGURLA MANIK REDDY; RANGISETTY JAGADEESH BABU; NANDAKUMAR MECHERIL VALSAN
权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD
摘要:The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.

专利号:US-9365544-B2
优先权日:2012-07-16
标题 :Process for the preparation of intermediates for the synthesis of Dabigatran Etexilate, and crystalline forms of said intermediates
发明人：HERNÀNDEZ GALLEGO SANTOS; MARQUILLAS OLONDRIZ FRANCISCO; POMARES MARCO MARTA
权利人:INTERQUIM SA
摘要:The present invention relates to new processes for the preparation of synthesis intermediate products useful in the preparation of Dabigatran Etexilate on an industrial scale. The invention also relates to new crystalline forms of intermediate products thus obtained.

专利号:WO-0061545-A1
优先权日:1999-04-14
标题 :Methods for solid phase combinatorial synthesis of integrin inhibitors
发明人：GOPALSAMY ARIAMALA; YANG HUI YU
权利人:AMERICAN HOME PROD
摘要:Compounds of the formula (I) are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula (I) are also provided.

专利号:US-9273030-B2
优先权日:2012-04-02
标题 :Process for the preparation of benzimidazole derivatives and salts thereof
发明人：THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; RAGHURAM SURAPARAJU
权利人:MSN LAB PRIVATE LTD
摘要:Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.