【药物名称】
化学结构式(Chemical Structure):
参考文献No.650611
标题:Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor
作者:Christiansen, L.B.; Weckens, M.; Bury, P.S.; Gissel, B.; Hansen, B.S.; Thorpe, S.M.; Jacobsen,P.; Kanstrup, A.; Jorgensen, A.S.; Naerum, L.; Wasserman, K.
来源:Bioorg Med Chem Lett 2002,12(1),17
合成路线图解说明:

The previously described 4-hydroxyphenyl chromane derivative (I) was converted to the 4-sulfanylphenyl analogue (IV) via the following sequence. Condensation of the sodium salt of phenol (I) with N,N-dimethylthiocarbamoyl chloride gave the O-aryl thiocarbamate (II), which underwent further thermal rearrangement to the S-aryl thiocarbamate (III) in diphenyl ether at 260 C. Reductive cleavage of thiocarbamate (III) using LiAlH4 gave rise to thiophenol (IV). Subsequent alkylation of (IV) with N-(2-chloroethyl)pyrrolidine (V) yielded thioether (VI). The methyl ether function of (VI) was then cleaved by heating with pyridine hydrochloride, and the resultant compound was finally isolated as the corresponding hydrochloride salt.

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