| 摘要 |
Use of 1-hydroxy-2-alkoxycarbonyl tetralin derivs. of formula (I) for prepn. of 2-amino- or 2-aminomethyl tetralin derivs. of formula (IV) is new. (IV) is prepd. by: (a) hydrolysing the ester gp. of (I) under basic conditions and eliminating the 1-OH gp. by hydrogenolysis in any order; followed by (b) Curtius reaction; or (c) hydrolysis of the ester gp. followed by introduction of a 2-isocyanate gp; (d) intramolecular formation of an oxazolidinone; and (e) hydrolysis in acid medium to give (IV; m = 0) and (f) hydrogenolysis of the 1-OH, formation of amide and redn. of the carbonyl gp. to CH2 to give (IV; m = 1). The configuration of position 1 and 2 is (1S, 2S) or (1R, 2R). R1 = Me or H; R = 1-4C alkyl. (I) are new. Intermediates of formula (V) are new, the configuration is as above.
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