C(3) AURATED 1,4-BENZODIAZEPIN-2-ONES - SYNTHESIS AND CHARACTERIZATION - CRYSTAL-STRUCTURE OF (L)AU[P(C6H4CH3-4)(3)] (HL = YDRO-1-METHYL-5-PHENYL-2H-1,4-BENZODIAZEPIN-2-ONE, DIAZEPAM)

The synthesis of a series of gold(I) metallated derivatives of some 1, 4-benzodiazepin-2-ones is described. They include mononuclear (L)Au(PR 3) (R = C6H5, C6H4CH3-4 or C2H5) as well as dinuclear species (L)Au(Ph 2P(CH2) PPh2)Au(L), n = 2, 3 (HL = ydro-1-methyl-5-phenyl-2H-1,4-benzo diazepin-2-one, DIAZEPAM or )-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepi n-2-one, PRAZEPAM). The deprotonated ligand is bonded to the AuPR3 moi ety through the C(3) atom. Activation of the C(sp(3))-H bond is achiev ed by means of a strong base in the presence of the phosphinegold chlo ride intermediate. The structure of (L)Au[P(C6H5CH3-4)(3)] has been de termined by X-ray diffraction. Some aspects of the reactivity of the m etallated species is also reported. (C) 1998 Elsevier Science S.A.