发明名称 METHOD OF PRODUCING 3,4-DIHYDROPROLINES AND 3,4-DEHYDROPIPERIDINES
摘要 The invention relates to a method for producing compounds of the general formula (I) in which R is hydrogen, C 1 -C 6 -alkoxy, -NHC 1 -C 6 -alkyl, -N(C 1 -C 6 -alkyl) 2, OH, NH 2 ; R 1 is hydrogen, C 1 -C 6 -alkyl, Me 3 Si, C 1 -C 6 -alkyl-S; R 2 is Boc, C1 -C 6 -acyl, mesyl, benzolsulfonyl, tosyl, trifluoroacetyl, A1-A3- peptide; n is 1, 2; and R 4 is H, C 1 -C 6 -alkyl rest. According to said method a pyrroline or dehydropiperidine derivative of the general formula (II) is reacted with a strong base and a compound of the general formula (III), in which Y is Cl, C 1 -C 6 -alkoxy, -NHC 1 -C 6 -alkyl, -N(C 1 -C 6 -alkyl) 2, N(C 1 -C 6 -alkyl) OC 1 -C 6, where R is not equal OH, or with carbon dioxide when R = OH. The reaction product of (II) and (III) is possibly hydrolyzed or reacted with a compound of the general formula (IV) R 1 -X, in which X is Cl, Br, I, MesO, TosO, triflate, R 1 is hydrogen, C 1 -C 6 -alkyl, Me 3 Si, C 1 -C 6 -alkyl-S or NH 4, or R 1 -X is (C 1 -C 6 -alkyl-'S) 2.
申请公布号 KR20010104730(A) 申请公布日期 2001.11.26
申请号 KR20017012187 申请日期 2001.09.25
申请人 发明人
分类号 C07D211/78;C07D207/16;C07D207/20;C07D211/70 主分类号 C07D211/78
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