http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-078788-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dbaced0995cda76fea038c684318a8fe |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/B01J23-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
filingDate | 2010-10-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2011-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-078788-A1 |
titleOfInvention | METHOD TO PREPARE DERIVATIVES OF 3,4-DIHYDROPIRAZIN [2,3-B] PIRAZIN-2 (1H) -ONA, INTERMEDIARIES OF SUCH SYNTHESIS AND PROCESS TO PREPARE THEM |
abstract | Claim 1: A method of preparing a compound of the formula (1), the method comprises contacting a compound of the formula (2) with R1-Y in a solvent, in the presence of a palladium catalyst, wherein said contact occurs under suitable conditions to provide a compound of formula 1, wherein: X is halogen, B (OR +) 2 or Sn (R ++) 3; Y is halogen, triflate, B (OR +) 2 or Sn (R ++) 3; where a) when X is halogen, then Y is B (OR +) 2 or Sn (R ++) 3; or b) when Y is halogen or triflate, then X is B (OR +) 2 or Sn (R ++) 3; wherein each R + is independently hydrogen or C1-3 substituted or unsubstituted alkyl, or each R +, together with the boron atom and the atoms to which they are attached, form a cyclic boronate; and R ++ is a C1-4 alkyl; and wherein R1 is C1-8 substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, or substituted or unsubstituted heterocyclyl alkyl; R2 is H, C1-8 substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclyl alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted cycloalkylalkyl; R3 and R4 are each independently H, C1-8 substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclyl alkyl, substituted or unsubstituted aralkyl, substituted cycloalkylalkyl or unsubstituted, or R3 and R4, together with the atom to which they are attached, form a substituted or unsubstituted cycloalkyl or substituted or unsubstituted heterocyclyl; or R2 and one of R3 and R4, together with the atoms to which they are attached, form a substituted or unsubstituted heterocyclyl; as long as the compound is not 6- (4-hydroxyphenyl) -4- (3-methoxybenzyl) -3,4-dihydropyrazino [2,3-b] pyrazin-2 (1H) -one, 6- (4- ( 1H-1,2,4-triazol-5-yl) phenyl) -3- (cyclohexylmethyl) -3,4-dihydropyrazino [2,3-b] pyrazin-2 (1H) -one, or (R) -6 - (4- (1H-1,2,4-triazol-5-yl) phenyl) -3- (cyclohexylmethyl) -3,4-dihydropyrazino [2,3-b] pyrazin-2 (1H) -one. |
priorityDate | 2009-10-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 39.