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公开(公告)号：US07312329B2
公开(公告)日：2007-12-25
申请号：US11004755
申请日：2004-12-03
IPC分类号： C07F9/02 , C07D239/02
CPC分类号： C07D239/42 , Y02P20/55
摘要： An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
摘要翻译： 提供了制备嘧啶衍生物的改进方法，包括使通式为Wittig试剂反应其中R为1至10个碳原子的烷基，芳基或芳基烷基，R 1是被取代或 未取代的烃基，R 2和R 3相同或不同，为氢或取代或未取代的烃基; Z可以被甲酰基，乙酰基，丙酰基，丁酰基，异丁酰基，戊酰基，异戊酰基，被磺酰基或烷基磺酰基取代的氨基，和被烷基，氨基或烷基氨基取代的磺酰基取代的硫，氧，磺酰基或亚氨基，X是卤素 ; 与其中R 4为氢的通式的醛，能够形成无毒的药学上可接受的盐的低级烷基或阳离子和每个R 5相同 或不同的是氢或可水解保护基团，或每个R 5与每个键合的氧原子一起形成可水解的环保护基团，或每个R 5， SUP>键合到与每个氧原子键合的相同取代基以形成可水解保护基团; 在一个基地的存在。
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公开(公告)号：US20050124639A1
公开(公告)日：2005-06-09
申请号：US11004755
申请日：2004-12-03
申请人： Narendra Joshi , Shekhar Bhirud , Batchu Chandrasekhar , K. Rao , Subhash Damle
发明人： Narendra Joshi , Shekhar Bhirud , Batchu Chandrasekhar , K. Rao , Subhash Damle
IPC分类号： C07D239/42 , A61K31/513 , A61K31/505 , C07D239/34
CPC分类号： C07D239/42 , Y02P20/55
摘要： An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
摘要翻译： 提供了制备嘧啶衍生物的改进方法，包括使通式为Wittig试剂反应其中R为1至10个碳原子的烷基，芳基或芳基烷基，R 1是被取代或 未取代的烃基，R 2和R 3相同或不同，为氢或取代或未取代的烃基; Z可以被甲酰基，乙酰基，丙酰基，丁酰基，异丁酰基，戊酰基，异戊酰基，被磺酰基或烷基磺酰基取代的氨基，和被烷基，氨基或烷基氨基取代的磺酰基取代的硫，氧，磺酰基或亚氨基，X是卤素 ; 与其中R 4为氢的通式的醛，能够形成无毒的药学上可接受的盐的低级烷基或阳离子和每个R 5相同 或不同的是氢或可水解保护基团，或每个R 5与每个键合的氧原子一起形成可水解的环保护基团，或每个R 5， SUP>键合到与每个氧原子键合的相同取代基以形成可水解保护基团; 在一个基地的存在。
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