http://rdf.ncbi.nlm.nih.gov/pubchem/patent/NZ-560972-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c524179979207d2c854b061e857d0c4d |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D411-04 |
filingDate | 2005-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_719ea2155d3c05af15f6ce082f400051 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_68a2f2d1f43b1f048fc14dc887d32642 |
publicationDate | 2009-07-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | NZ-560972-A |
titleOfInvention | Process and methods for the preparation of optically active cis-2-hydroxymethyl-4-(cytosin-1' -yl)-1,3-oxathiolane or pharmaceutically acceptable salts thereof |
abstract | Disclosed is a process for producing an optically active 1,3-oxathiolane derivative of formula I or II, wherein: R1 is H, C1-6alkyl, C6-12aryl, C6-12arylalkyl, (CO)C1-6alkyl, (CO)O-C1-6alkyl, (CO)C6-12aryl, or (CO)C6-12arylalkyl; R2 is H, C1-6alkyl or CO-R5; R3 is H, C1-6alkyl, bromide, chloride, fluoride, iodide or CF3; and R5 is H or C1-6alkyl; wherein in the definitions of R1, R2, R3 and R5 "alkyl" is, in each case, unsubstituted or substituted by one or more of halogen, nitro, nitroso, sulfate, sulfate ester, sulfonate, sulfonate ester, phosphonate ester, amide, C1-6alkyl, C6-12aralkyl, C6-12aryl, C1-6alkyloxy, C6-12aryloxy, C(O)-C1-6alkyl, C(O)-C6-12aryl, C(O)C6-12aralkyl, heterocycle having 3-10 ring members, hydroxyl, amino, ester, cyano, azido, amidino or guanido; and in the definitions of R1, R2, R3 and R5 "aryl" is, in each case, unsubstituted or substituted by one or more of halogen, nitro, nitroso, sulfate, sulfate ester, sulfonate, sulfonate ester, phosphonate ester, amide, C1-6alkyl, C6-12aralkyl, C6-12aryl, C1-6alkyloxy, C6-12aryloxy, C(O)-C1-6alkyl, C(O)-C6-12aryl, C(O)C6-12aralkyl, heterocycle having 3-10 ring-members, hydroxyl, amino, ester, cyano, azido, amidino or guanido; said process comprising: a) reacting a compound of formula III (in the cis configuration) with a chiral acid to produce two diastereomeric salts, wherein said chiral acid is (1R)-(-)-10-camphorsulfonic acid, (-)-2,3-dibenzoyl-L-tartaric acid, (+)-L-tartaric acid or (-)-L-malic acid; b) recovering substantially one diastereomeric salt; c) converting said one diastereomeric salt into said optically active compound. |
priorityDate | 2005-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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