| 摘要 |
<p>Prepn. of cpds. having the general formula (I): (where r1 is 1-5C alkyl and R2 and R3 are same or different gps. of formula (II): in which R4, R5 and R6 and same or different H, F, Cl, Br, 1-3C alkyl or alkoxy, -NO2 or -CF3, but no more than one of R4, R5 and R6 is -NO2, -NO2, -CF3, branches alkyl or alkoxy, and R1 is 2-5C alkyl if R2 and R3 are Ph) by the process: R1NH-CR2=CH- -R3 + HNCO ring-closure inert organic solvent right arrow (I) -20 degrees C to +35 degrees C (pref. -5 degrees to +15 degrees C) Cpds. (I) are tranquilisers-sedatives/hypnotics and CNS-depressants. (60-2000 mg/day in 2-4 doses of 15-1000 mg). Cpds (Ib) having the formula (where R2k and R3k are same or different gps. of formula where R4k is H, F, Cl or Br) are useful as sleeping drugs (120-2000 mg. at bed-time). Cpds (I) with unsubstd. Ph in positions 4 and 6 are useful as anti-inflammatory agents (110-2000 m/day). HNCO is unstable and is used as MOCN (where M is a cation) in an acid medium.</p> |
