| PATENT ASSIGNEE'S COUNTRY | UK |
| UPDATE | 07.00 |
| PATENT ASSIGNEE | This data is not available for free |
| PATENT CLAIMS |
Process for prepn of (S)-4-{[3-[2(dimethylamino)ethyl]-1H- indol-5-yl]methyl}-2-oxazolidinone - Forming a carbamate from Me 4-nitro-(L)-phenylalaninate HCl represented by O2N-C6H4-CH2-CH(CO2Me)-NH2.HCl (I); by adding Na2 CO3 & n-Bu chloroformate & reacting to give methyl(S)-N- butoxycarbonyl-4-nitrophenylalaninate, represented by O2N-C6H4-CH2-CH(CO2Me)-NH-CO2Bu (II) - Reducing (II) to give methyl (S)-N-butoxycarbonyl-4-amino phenylalaninate, represented by H2N-C6H4-CH2-CH(CO2Me)-NH-CO2Bu (III) - Reducing the Me ester grouping -CO2Me in (III) to give (S) N-butoxycarbonyl-4-aminophenylalaninol represented by H2N-C6H4-CH2-CH(CH2OH)-NH-CO2Bu (IV) - Ring closure of (IV) without the need for phosgene to give (S)-4-(4-aminobenzyl)-2-oxazolidinone (V) - Prepn of the diazonium salt of (V) followed by reduction without the need for Sn chloride to give the hydrazine (S) 4-(4-hydrazinobenzyl)-2-oxazolidinone hydrochloride (VI) - Fischer reaction of (VI) |
| PATENT PHOTOCOPY | Available on request |
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