α,β-unsaturated acyl-substituted imido derivatives are a kind of important electron-deficient alkenes and widely applied in synthesis.In this paper,a new synthetic method of these alkenes is developed and the cataly...α,β-unsaturated acyl-substituted imido derivatives are a kind of important electron-deficient alkenes and widely applied in synthesis.In this paper,a new synthetic method of these alkenes is developed and the catalytic mechanism is discussed.With LiCl as the catalyst,the products are synthesized with succinimides or phthalimide、crotonic anhydride in the present of triethylamine at low temperature.The reactions proceed smoothly in the given condition with good yields.展开更多
Aim To synthesize the tripepide Weinreb amide Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) as a useful precursor of aspartyl peptide aldehyde derivatives; Methods DCC, IBCF method was used for preparation of ...Aim To synthesize the tripepide Weinreb amide Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) as a useful precursor of aspartyl peptide aldehyde derivatives; Methods DCC, IBCF method was used for preparation of Weinreb amide; N hydroxysuccinimide activated ester was used in peptide synthesis; and Boc as N protecting group of amino acid. Results Boc Asp(OBzl) N(OMe)Me (3), Boc β Ala Asp(OBzl) N(OMe)Me (5), and Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) were synthesized successfully. Conclusion An useful precursor of tripeptide aspartyl aldehydes was synthesized.展开更多
文摘α,β-unsaturated acyl-substituted imido derivatives are a kind of important electron-deficient alkenes and widely applied in synthesis.In this paper,a new synthetic method of these alkenes is developed and the catalytic mechanism is discussed.With LiCl as the catalyst,the products are synthesized with succinimides or phthalimide、crotonic anhydride in the present of triethylamine at low temperature.The reactions proceed smoothly in the given condition with good yields.
文摘Aim To synthesize the tripepide Weinreb amide Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) as a useful precursor of aspartyl peptide aldehyde derivatives; Methods DCC, IBCF method was used for preparation of Weinreb amide; N hydroxysuccinimide activated ester was used in peptide synthesis; and Boc as N protecting group of amino acid. Results Boc Asp(OBzl) N(OMe)Me (3), Boc β Ala Asp(OBzl) N(OMe)Me (5), and Boc Asp(OBzl) β Ala Asp(OBzl) N(OMe)Me (7) were synthesized successfully. Conclusion An useful precursor of tripeptide aspartyl aldehydes was synthesized.
