| 摘要 |
<p>PURPOSE:To provide a new alpha-guanidino acid derivative useful for selectively amidinating the N-terminal of a peptide under mild conditions. CONSTITUTION:The compound of formula I [R1 is substituted benzenesulfonyl bearing 1 to 5 methyl or methoxy groups on the benzene ring; R2 is a side chain obtained by protecting, with a protective group, the side chain or the functional group(s) therein of Ala, Val, Leu, Ile, Nle, Gln, Asn, Phe, Met, Met(O), Met(O2), Ser, Tyr, Thr, Glu, Asp, Lys, Orn, Cys, Trp, His or Arg] or formula II (R3 is H, OH or protected OH; n is 1 or 2), e.g. N-p- toluenesulfonylamidinoisoleucine. The compound of the formula I can be obtained by treating a compound of formula III with concentrated ammonium water. And, the compound of the formula II can be obtained from a compound of formula IV by a similar treatment.</p> |
