中国药物化学杂志
中國藥物化學雜誌
중국약물화학잡지
Chinese Journal of Medicinal Chemistry
2001年
1期
45-46
,共2页
武引文%梅和珊%张忠敏%吕新英%颜廷仁
武引文%梅和珊%張忠敏%呂新英%顏廷仁
무인문%매화산%장충민%려신영%안정인
莫索尼定%合成%硝化%还原
莫索尼定%閤成%硝化%還原
막색니정%합성%초화%환원
以乙脒盐酸盐为原料,经环合硝化、氯化、还原、加成脱水、醇解成盐合成了中枢性降压药莫索尼定,总产率为24.8%。在氯化反应中,以三氯氧磷为氯化剂,产率为92.8%。在还原反应中,以铁粉为还原剂,完成反应后进行水蒸气蒸馏,产率为87.7%。
以乙脒鹽痠鹽為原料,經環閤硝化、氯化、還原、加成脫水、醇解成鹽閤成瞭中樞性降壓藥莫索尼定,總產率為24.8%。在氯化反應中,以三氯氧燐為氯化劑,產率為92.8%。在還原反應中,以鐵粉為還原劑,完成反應後進行水蒸氣蒸餾,產率為87.7%。
이을미염산염위원료,경배합초화、록화、환원、가성탈수、순해성염합성료중추성강압약막색니정,총산솔위24.8%。재록화반응중,이삼록양린위록화제,산솔위92.8%。재환원반응중,이철분위환원제,완성반응후진행수증기증류,산솔위87.7%。
Moxonidine is known as the central hypotensor of the secondarygeneration.It was synthesized from acetamidine hydrochloride as the starting material via cyclization,nitration,chlorination,reduction,addition and dehydration,alcoholysis and salt formation.The overal yield was 24.8%.The yield of chlorination was 92.8%,using phosphorus oxychloride as the chlorinating agent.The yield of reduction was 87.7%,using iron powder as the reducting agent and steam distillation as the separation method.