CH2(Coc)2 2( CH3)3COH C6H5N(CH3)2 -CH2ICooc(cH3 )32 304h (84%) HN(CH3)2 -CON(CH3 )2 (89%)
(84%) (89%) HN(CH3) 2 COCl CON(CH3) 2 30 ,4h 。 + 2 CH2[COOC(CH3) 3] 2 C6 H5 N(CH3) 2 CH2(COCl) 2 (CH3) 3 COH
4取代氨基吡啶催化剂 NR 2 2 ROH t Cox OR N O=C NRo R RCOOR ⊕NH nr2yJ-N( CH3)2,-N=C(NMe2)2,-N
4-取代氨基吡啶催化剂 + N NR2 RCOX R'OH N NR2 O C R H OR' RCOOR' + N H NR2 X -NR2为-N(CH3 )2 , -N=C(NMe2 )2 , N
酸酐作酰化剂 CH3 H3C (CF3CO)2O 混合酸酐法 H3C一 COoH HO r t. 10min CH C CH3 H3C (97%) CH3 H3C C CH3(CH2 )2-CH-COOH +t-BuOH+CI CH CH3)2N CH3(CH2)2-CH-COOBu-t 15h CH3(95%)
•酸酐作酰化剂 H3C CH3 CH3 COOH + HO H3C H3C (CF3CO) 2O r.t. 10min H3C H3C COO CH3 CH3 H3C CH3(CH2) 2 CH COOH CH3 + t BuOH+Cl COCl Cl Cl CH3(CH2) 2 CH COOBu CH3 t (CH3) 2N N 1.5h (97%) (95%) 混 合 酸 酐 法
羧酸作酰化剂 DCC脱水法(二环己基碳化二亚胺) O R-C NEC=N NH >R-C-0-C O -R-C-0-R+-N-C-N
•羧酸作酰化剂 DCC脱水法(二环己基碳化二亚胺) + N H N H C O R C O O C NH N R C O O H + N C N + R' O H R C O O R
羧酸作酰化剂 活性羧酸酯法(肽类,大环內酯类合成) (1)羧酸硫醇酯 RCOoH t ph3P NS-S′N Ph3P=O NS-C-R
•羧酸作酰化剂 活性羧酸酯法(肽类，大环内酯类合成) (1)羧酸硫醇酯 RCOOH + N S S N + Ph3 P N S C R O + Ph3 P O