| 摘要 |
<p>1310046 Thiazacyclic amino compounds CIBA-GEIGY AG 2 July 1970 [8 July 1969 27 Nov 1969] 32141/70 Heading C2C The invention comprises the novel compounds 6 - amino - 2,2 - dimethyl - 3 - (2,2,2 - trichloroethoxy - carbonylamino) - penam, 6 - amino- 2,2 - dimethyl - 3 - 4 - methoxybenzyloxycarbonyl - amino) - penam, 6 - amino - 3 - (2- iodoethoxycarbonylamino) - 2,2 - dimethylpenam, and 3 - acetoxymethyl - 7 - amino - 4- (2,2,2 - trichloroethoxycarbonylamino) - ceph- (2)em, and a process for preparing these compounds and compounds of the formula wherein X is an etherified hydroxyl group, and R is a methylene group which may be substituted by one or two optionally substituted methyl groups, or a vinylene group which contains an optionally substituted methyl group attached to the carbon atom of the vinylene group which in the sulphur-nitrogen ring is exclusively bound to ring carbon atoms by reacting compounds of the formula in which Ac 0 is the acyl radical of an organic carboxylic acid, with acid halides capable of forming imide halides, converting the resulting imide halides into the corresponding imino ethers by treatment with alcohols and splitting the resulting imino ethers by treatment with a hydroxy compound, and, if desired, replacing in the resulting compounds having aliphatically bound chlorine or bromine atoms in the radical X, such Cl or Br atoms by treatment with iodine salts, and/or, if desired, resolving resulting isomer mixtures into single isomers. The following intermediates are prepared: 2,2 - dimethyl - 6 - (phenylacetylamino) - 3- (2,2,2 - trichloroethoxycarbonylamino)- penam, 2,2 - dimethyl - 6 - (phenylacetylamino)- penam- 3 - carboxylic acid azide, 3 - isocyanato - 2,2- dimethyl - 6 - (phenylacetyl - amino) - penam, 3 - (4 - benzyloxycarbonylamino)- 2,2 - dimethyl- 6 - (phenylacetylamino) - penam, 3 - (2 - iodoethoxycarbonylamino) - 2,2 - dimethyl - 6 - (phenylacetylamino) - penam, 3 - (2 - bromoethoxycarbonylamino) - 2,2 - dimethyl - 6 - (phenylacetylamino) - penam, 2,2 - dimethyl - 6 - (phenoxyacetylamino) - 3 - (2,2,2 - triohloroethoxycarbonylamino) - penam, penicillin - V - azide, 3 - isocyanato - 2,2 - dimethyl - 6 - (phenoxyacetylamino) - penam, 2,2 - dimethyl - 3 - (phenacyloxycarbonylamino)- 6 - (phenylacetylamino)- penam, 3 - acetoxymethyl - 7 - (2 - thienylacetylamino) - 4 - (2,2,2 - trichloroethoxycarbonylamino) - ceph(2)em, 6 - (tert - butoxycarbonylamino) - 2,2 - dimethyl - 3 - (2,2,2 - trichloroethoxycarbonylamino)- penam, 2,2 - dimethyl- 3 - (4 - methoxybenzyloxycarbonylamino)- 6- (phenoxyacetylamino)- penam, and 6 - (chlorocarbonylamino) - 2,2 - dimethyl - 3 - (2,2,2- trichloroethoxycarbonylamino)-penam,</p> |
