http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0815102-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d202e9e866984fe229f6facc38f1d740 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06 |
| filingDate | 1996-03-11^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8f0633afcc15df184a08c5d7b3b38406 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5989eaafe8ab318aede35d84280fa610 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c7b3af85bbaf6e981457bb5f0d0e58dd |
| publicationDate | 1998-01-07^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-0815102-A1 |
| titleOfInvention | REDUCTIVE ALKYLATION PROCESS FOR THE PREPARATION N-(2-(R)-HYDROXY-1-(S)-INDANYL)-2(R)-PHENYLMETHYL-4(S)-HYDROXY-5-(1-(4-(3-PYRIDYLMETHYL)-2(S)-N'-(t-BUTYLCARBOXAMIDO)-PIPERAZINYL))-PENTANEAMIDE (=COMPOUND J OR L-735,524) |
| abstract | A process of reductive amination efficiently yields an HIV protease inhibitor. The invention described herein concerns the final bond-forming step in the synthesis of the HIV protease inhibitor (J). In the invention, the penultimate intermediate (1) is converted to (J) via introduction of a 3-picolyl moiety in the form of 3-pyridinecarboxaldehyde (2) via a reductive alkylation. A process for synthesizing compound (J) of structure (3) comprising the steps of: (a) reacting for at least 5 minutes in suitable solvent one equivalent of the compound having structure (4) with excess 3-pyridine carboxaldehyde in the presence of excess reducing agent, at a temperature range of between about -78 °C and about 90 °C; (b) to give compound (J) or hydrate thereof. |
| priorityDate | 1995-03-15^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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