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【答案】应助回帖
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220chengeng: 金币+2, 感谢应助，辛苦。 2012-12-01 21:38:12
fuxd525: 金币+25, 翻译EPI+1, ★★★很有帮助 2012-12-04 08:53:32
Carena: 金币+10, 金币代发 2013-01-12 22:07:17
以吗啡啉和3,4-二氟硝基苯为原料，经取代，还原，重氮化-卤化反应合成中间体3-氟-4-吗啉基溴苯(4)；以(R)-环氧氯丙烷、氰酸钾、邻苯二甲酰亚胺钾盐为原料合成中间体(R)-5-邻苯二甲酰亚胺甲基-2-噁唑烷酮(6)。然后对(4)和(6)进行缩合、水解合成利奈唑胺。总收率由文献报道的11%左右提高至26%。该合成工艺提高了反应收率，降低了生产成本，有利于工业化生产。
It can synthetize intermediates 3 - fluorine - 4 - morpholine base bromobenzene(4) through substitution, reduction and diazotization - halogenating reaction with morphine Lin and 3, 4 - two fluorine nitrobenzene；Also，It can synthetize the intermediates (R)-5-adjacent benzene 2 formyl imine methyl - 2 - oxazole hydride ketone(6)with (R)-epoxy chloropropane, potassium cyanate, adjacent benzene 2 formyl imine potassium。Then produce Nye azole amine through condensation, hydrolysis with (4) and (6)。There are literatures reported that total aromatics increased from 11% to 26%。This synthesis process can not only improve rate of reaction and reduce the cost，but also benefit industral production。 |
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