- Diastereoselective synthesis of a core fragment of ritonavir and lopinavir
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A novel approach to the synthesis of Boc-core, a key starting material for ritonavir and lopinavir involving an unprecedented diastereoselective nitroaldol reaction on β-amino aldehyde is disclosed.
- Roy, Arnab,Reddy, Lekkala Amarnath,Dwivedi, Namrata,Naram, Jyothirmayi,Swapna, Rodda,Malakondaiah, Golla China,Ravikumar, Mylavarpu,Bhalerao, Dinesh,Pratap, Taduri Bhanu,Reddy, Padi Pratap,Bhattacharya, Apurba,Bandichhor, Rakeshwar
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scheme or table
p. 6968 - 6970
(2012/02/13)
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- A PROCESS FOR THE SYNTHESIS OF 2-AMINO-5-PROTECTED AMINO-3-HYDROXY-1, 6-DIPHENYLHEXANE OR A SALT THEREOF - AN INTERMEDIATE FOR ANTIVIRAL DRUGS
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The present invention relates to an improved process for preparing 2-amino-5-protected-amino-3-hydroxy-1,6-diphenylhexane compounds or acid addition salts thereof, which can be useful intermediates for preparing compounds with antiviral activity. The present invention further provides a process for preparing HIV protease inhibitors, lopinavir and ritonavir.
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Page/Page column 20
(2008/06/13)
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- HIV protease inhibiting compounds
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A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
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Page/Page column 156
(2010/02/12)
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- Retroviral protease inhibiting compounds
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A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
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- RETROVIRAL PROTEASE INHIBITING COMPOUNDS
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A compound of the formula: STR1 is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
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- Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane
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Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: STR1 wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from STR2 wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and STR3 wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7a OC(O)--wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are STR4 wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.
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