| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d313dce6b318f9cc1ab4dcebd2003fdf |
| classificationCPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C213-08 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D303-36
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C215-28
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B53-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C217-60 |
| filingDate |
1995-10-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4372acb3caf0c2742d20c7ce9ac23823
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_336618171ba82f47a5da9c393a697f83
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c1b642713fd90670ffe08cc7550a8ed2 |
| publicationDate |
1996-06-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
WO-9617821-A1 |
| titleOfInvention |
Process for the preparation of enantiomerically pure (s,s) aminoepoxides, key intermediates for hiv protease inhibitors, via their chlorohydrines |
| abstract |
Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of formula (1) wherein R?1 and R2¿ are amino protective groups and R3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of formula (2) wherein R?1, R2 and R3¿ are as defined hereinbefore with (chloromethyl)lithium at -20 °C or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-1,2(S)-epoxy-4-phenyl-butane. |
| isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1148046-A1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6683214-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-100339831-B1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1777213-A1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2011061590-A1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6127556-A
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1148046-A4 |
| priorityDate |
1994-12-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |