| 摘要 |
Preparation of gamma -lactams (I) comprises cyclizing the corresponding amino-amide (II). Preparation of gamma -lactams of formula (I) comprises cyclizing an amino-amide of formula (II). R1 = H; 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 2-8C alkoxyalkyl or 1-8C acyl (optionally substituted by 1 or more halo or N- O-, P-, or S- containing group), 3-7C optionally unsaturated cycloalkyl (optionally containing heteroatoms (e.g. N, O, P or S) and optionally substituted by 1 or more 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 1-8C acyl, 1-8C alkoxy or 2-8C alkoxyalkyl (themselves optionally substituted by 1 or more halo or N- O-, P-, or S- containing group)); aryl (e.g. phenyl or naphthyl), aralkyl (e.g. benzyl or phenethyl), heteroaryl (e.g. furyl, pyrrolyl or pyridyl) or heteroaralkyl (e.g. furfuryl, pyrrolylmethyl, pyridylmethyl, furylethyl, pyrrolylethyl or pyridylethyl) (all optionally substituted by 1 or more 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 1-8C acyl, 1-8C alkoxy or 2-8C alkoxyalkyl (themselves optionally substituted by 1 or more halo or N- O-, P-, or S- containing group)); or N-bonded amino acid or peptide residue; R2 = H; 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl or 2-8C alkoxyalkyl (optionally substituted by 1 or more halo or N- O-, P-, or S- containing group), 3-7C optionally unsaturated cycloalkyl (optionally containing a heteroatom (e.g. N, O, P or S) and optionally substituted by 1 or more 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 1-8C acyl, 1-8C alkoxy or 2-8C alkoxyalkyl (themselves optionally substituted by 1 or more halo or N- O-, P-, or S- containing group)); aryl (e.g. phenyl or naphthyl), aralkyl (e.g. benzyl or phenethyl), heteroaryl (e.g. furyl, pyrrolyl or pyridyl) or heteroaralkyl (e.g. furfuryl, pyrrolylmethyl, pyridylmethyl, furylethyl, pyrrolylethyl or pyridylethyl) (all optionally substituted by 1 or more 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, 1-8C acyl, 1-8C alkoxy or 2-8C alkoxyalkyl (themselves optionally substituted by 1 or more halo or N- O-, P-, or S- containing group)); R3 = H, ClCO, 1-8C acyl, C-bonded amino acid or peptide residue or a peptide protecting group such as formyl, carbamoyl, benzyloxycarbonyl, t-butyloxycarbonyl, allyloxycarbonyl or trifluoracetyl; X = halo or sulfonic acid ester. Independent claims are included for: (1) intermediates of formula (II), (IV) and (V) and their salts; and (2) use of (II), (IV) and (V) and their salts as intermediates for bioactive compounds. R4 = 1-8C alkyl, 2-8C alkenyl, 1-8C alkoxy or 2-8C alkenyloxy (optionally substituted by 1 or more halo); aryl (e.g. phenyl or benzyl), aralkyl (e.g. benzyl or phenethyl) or aralkyloxy (e.g. benzyloxy); R5 = H or combines with R3 to form a ring. |
