| 摘要 |
1. A process for making HIV protease inhibitor of the structure comprising the steps of: (a) heating for at least one hour a mixture of one equivalent of (S)-4-(3-picolyl)-2-tert-butylcarboxamide piperazine (1) with about one equivalent of at a temperature range between about 25 degree C and about 150 degree C, said mixture optionally containing suitable solvent; (b) deblocking the compound 3 by treatment with acid (c) neutralizing the acid. 2. The process of Claim 1, wherein the temperature range is between about 50 degree C and about 120 degree C. 3. The process of Claim 1, wherein the temperature range is between about 65 degree C and about 85 degree C. 4. The process of Claim 1, wherein the suitable solvent is either an ester, an alcohol, a hydrocarbon, an ether or a formamide, or mixture thereof. 5. The process of Claim 1, wherein the suitable solvent is an alcohol. 6. The process of Claim 1, wherein the suitable solvent is methanol or isopropanol. 7. The process of Claim 1, wherein the deblocking of step (b) is carried out with gaseous HC1. 8. The process of Claim 1 for synthesis of a compound of the structure comprising the steps of: (a) heating for at least one hour a mixture of one equivalent of (S)-4-(3-picolyl)-2-tert-butylcarboxamide piperazine (1) with about one equivalent of at a temperature range between about 65 degree C and about 85 degree C, said mixture optionally containing as solvent methanol or isopropanol or mixture thereof; (b) cooling the mixture to about 0 degree C; (c) deblocking the compound 3 with gaseous HC1 (d) neutralizing with NaOH. 9. The compound (S)-4-(3-picolyl)-2-tert-butylcarboxamide piperazine (1) |
