|
【结 构 式】 
|
【药物名称】ST-1863 【化学名称】2-[3-[2-(4-Chlorophenyl)ethoxy]benzyl]malonic acid dimethyl diester 【CA登记号】 【 分 子 式 】C20H21ClO5 【 分 子 量 】376.84037 |
【开发单位】Sigma-Tau (Originator) 【药理作用】Antidiabetic Drugs, ENDOCRINE DRUGS, Lipoprotein Disorders, Treatment of , METABOLIC DRUGS, Type 2 Diabetes Mellitus, Agents for |
合成路线1
Knoevenagel condensation of 4-hydroxybenzaldehyde (I) with dimethyl malonate in the presence of pyridinium acetate affords the benzylidene malonate (II), which is further hydrogenated over Pd/C to furnish dimethyl (4-hydroxybenzyl)malonate (III). Then, Mitsunobu coupling between phenol (III) and 4-chlorophenethyl alcohol (IV) gives rise to the title compound.
| 【1】 Catini, R.; Brunetti, T.; Arduini, A.; et al.; New phenylalkylcarboxylate derivatives as hypoglycemic and hypolipidemic agents. Drugs Fut 2002, 27, Suppl. A. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 13433 | 4-Hydroxybenzaldehyde; p-Hydroxybenzaldehyde | 123-08-0 | C7H6O2 | 详情 | 详情 |
| (II) | 58897 | 2-[(4-Hydroxyphenyl)methylene] propanedioic acid dimethyl ester; 4-Hydroxy benzylidene malonic acid dimethyl ester; Dimethyl 2-[(4-hydroxyphenyl)methylene]propane dioate | 51947-45-6 | C12H12O5 | 详情 | 详情 |
| (III) | 58898 | dimethyl 2-(4-hydroxybenzyl)malonate | C12H14O5 | 详情 | 详情 | |
| (IV) | 33783 | 2-(4-chlorophenyl)-1-ethanol | 1875-88-3 | C8H9ClO | 详情 | 详情 |
Extended Information