摘要 |
PROBLEM TO BE SOLVED: To obtain a new thiocarbamic acid ester derivative high in safety, having an antihypercholesterolemia activity and useful for treating arteriosclerosis or the like. SOLUTION: A compound of formula I [R1 is H, a lower alkyl or the like; R2 is H, a lower acyl or the like; R3 is a (substituted) phenyl or a heterocycle; R4 is H, a halogen, a lower alkyl or the like; R5 and R6 are each H or a lower alkyl, or they are linked with each other to form a ring; Y is C or Si; G1 to G3 are each CH or N; (m) and (n) are each 0 or 1; E is CR7R8 (R7 and R8 are each H or a lower alkyl); F is a carbonyl l or CR9R10 (R9 and R10 are each H or a lower alkyl)], for example, N-methyl-N-[3-[2-[N'-methyl-N'-3- thienylmethyl)amino]ethoxy]phenyl]thiocarbamic acid O-(5-trimethylsilylpyridin-2- yl)ester. Further, a compound of formula I is obtained by reacting a halogenated thioformate of formula II (V is a halogen) with a compound of formula III in a solvent such as tetrahydrofuran in the presence of a base.
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