中国医药工业杂志
中國醫藥工業雜誌
중국의약공업잡지
CHINESE JOURNAL OF PHARMACEUTICALS
2010年
4期
241-243
,共3页
李凡%侯兴普%李林%律涛%杜玉民
李凡%侯興普%李林%律濤%杜玉民
리범%후흥보%리림%률도%두옥민
istradefylline%抗帕金森病药%腺苷A_(2a)受体拮抗剂%合成
istradefylline%抗帕金森病藥%腺苷A_(2a)受體拮抗劑%閤成
istradefylline%항파금삼병약%선감A_(2a)수체길항제%합성
istradefylline%antiparkinsonian agent%adenosine A_(2a) receptor inhibitor%synthesis
香草醛经甲基化、Knoevenagel缩合、氯化亚砜氯代得(E)-3,4-二甲氧基苯丙烯酰氯,再与1,3-二乙基-5,6-二氨基尿嘧啶(7)经酰胺化、闭环及甲基化反应制得抗帕金森病药istradefylline.7可由N,N'-二乙基脲和氰乙酸经缩合闭环、亚硝化及还原反应制得.总收率约54%(以N,N'-二乙基脲计).
香草醛經甲基化、Knoevenagel縮閤、氯化亞砜氯代得(E)-3,4-二甲氧基苯丙烯酰氯,再與1,3-二乙基-5,6-二氨基尿嘧啶(7)經酰胺化、閉環及甲基化反應製得抗帕金森病藥istradefylline.7可由N,N'-二乙基脲和氰乙痠經縮閤閉環、亞硝化及還原反應製得.總收率約54%(以N,N'-二乙基脲計).
향초철경갑기화、Knoevenagel축합、록화아풍록대득(E)-3,4-이갑양기분병희선록,재여1,3-이을기-5,6-이안기뇨밀정(7)경선알화、폐배급갑기화반응제득항파금삼병약istradefylline.7가유N,N'-이을기뇨화청을산경축합폐배、아초화급환원반응제득.총수솔약54%(이N,N'-이을기뇨계).
Istradefylline, the antiparkinsonian agent, was synthesized from vanillin via methylation, Knoevenagel condensation and chlorination by SOCl_2 to give (E) -3,4-dimethoxy cinnamoyl chloride, which was subjected to amidation with l,3-diethyl-5,6-diaminouracil (7), followed by cyclization and methylation. Compound 7 was prepared from N,N'-diethylurea and cyanoacetic acid by condensation, cyclization, nitrosation and reduction. The overall yield was about 54% (based on N, N'-diethylurea).
