专利号:US-11891375-B2 优先权日:2021-07-26 标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates 发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
专利号:US-12162849-B2 优先权日:2018-12-21 标题 :Synthesis of 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or of the methyl-d3 deuterated form thereof 发明人:HOVEYDA HAMID; DUTHEUIL GUILLAUME 权利人:OGEDA SA 摘要:The present invention relates to a method of synthesis of compound (I), wherein R1 represents methyl or methyl-d3, thus corresponding to 3-methyl-1,2,4-thiadiazole-5-carbohydrazide or to the methyl-d3 deuterated form thereof. These compounds are useful as key intermediates in the synthesis of pharmaceutical compounds, especially fezolinetant and deuterated fezolinetant.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:WO-2011116933-A1 优先权日:2010-03-24 标 题 :Process for the preparation of 2-substituted 4-amino-5-cyanopyrimidines 发明人:DICK VIKTOR; HANSELMANN PAUL; KRAMER RAINER; LADNAK VIKTOR 权利人:LONZA AG; DICK VIKTOR; HANSELMANN PAUL; KRAMER RAINER; LADNAK VIKTOR 摘要:A compound of the formula (I), wherein R 1 is C 1-4 alkyl or phenyl, is prepared by reacting a dicyanomethanide of the formula: M r n + [CH(CN) 2 ] rÌ… n (II), wherein M is an alkali or alkaline earth metal and r is 1 or 2, with carbon monoxide to obtain a dicyanoethenolate of the formula: M r n + [(NC) 2 C=CH–O] rÌ… (III), which is acylated to obtain an acyloxymethylenemalononitrile of the formula: (NC) 2 C=CH–OCOR 2 (IV), wherein R 2 is C 1-4 alkyl, which in turn is reacted with an amidine of the formula (V) to obtain the 4-amino-5-cyanopyrimidine of the formula (I). The compound of formula (I), wherein R is methyl, is an intermediate in a synthesis of thiamin (vitamin B 1 ).
专利号:US-8252927-B2 优先权日:2008-07-22 标题:Synthesis of substituted 4-amino-pyrimidines 发明人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD 权利人:KARGE REINHARD; LETINOIS ULLA; SHIEFER GERHARD; DSM IP ASSETS BV 摘要:The present invention is directed to a process for the manufacture of compounds of formula IV wherein R 1 is an amino protecting group, and R 2 is hydrogen or C 1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M + is a cation, preferably selected from the group consisting of Li + , Na+, K + , ½ Mg 2+ and ½ Zn 2+ , (formula 1 a ) with an ammonium salt NH 4 + X − , wherein X − is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R 2 —CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B 1 .
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合成参考文献
摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 124. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 117. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 190. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 184. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 207.