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16th May 2014 @ 02:28
Osm: OSM-S-211_to_OSM-S-220

Original Sources

Attempts:

http://malaria.ourexperiment.org/uri/54c 

GitHub Link

 

Biological Data

N/A

Synonyms

AEW 128

FC1=C(F)C=C([I+]C2=C([CH2+])C=C(C)C=C2C)C=C1

InChI=1S/C15H14F2I/c1-9-6-10(2)15(11(3)7-9)18-12-4-5-13(16)14(17)8-12/h4-8H,1-3H3/q+1

HTOMECXYWUWECF-UHFFFAOYSA-N

(3,4-difluorophenyl)(mesityl)iodonium triflate

Attached Files
8th May 2014 @ 05:28
Osm: OSM-S-211_to_OSM-S-220

OSM-S-220

Original Sources

Original synthesis of related compound found in MMV briefing document found in this post:A New Triazolopyrazine Series for OSM - Series 4

See OSM-S-219 for synthesis of related compound

Attempts:

Synthesis of 5-chloro-3-(4-chlorophenyl)-[1,2,4]triazolo[4,3-a]pyrazine (JU 8-1)

GitHub Link

 

Biological Data

Single Shot Potencies for Compounds Submitted to GSK

Synonyms

JU 8

ClC1=CN=CC2=NN=C(C3=CC=C(Cl)C=C3)N21

InChI=1S/C11H6Cl2N4/c12-8-3-1-7(2-4-8)11-16-15-10-6-14-5-9(13)17(10)11/h1-6H

VCWFDFYRPOTNNX-UHFFFAOYSA-N

5-chloro-3-(4-chlorophenyl)-[1,2,4]triazolo[4,3-a]pyrazine

Linked Posts
Attached Files
8th May 2014 @ 04:00
Osm: OSM-S-211_to_OSM-S-220

Original Sources

Original synthesis found in MMV briefing document found in this post:A New Triazolopyrazine Series for OSM - Series 4

Other attempts:

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-8)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-7)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-6)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-5)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-4)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-3)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-2)

Synthesis of 4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (JU 3-1)

 

Synthesis of 4-(5-chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-9)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-8)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-7)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-6)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-5)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-4)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-3)

4-(5-Chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 97-2)


GitHub Link

 

Biological Data

Single Shot Potencies for Compounds Submitted to GSK

Synonyms

AEW 97

JU 3

ClC1=CN=CC2=NN=C(C3=CC=C(C#N)C=C3)N21

InChI=1S/C12H6ClN5/c13-10-6-15-7-11-16-17-12(18(10)11)9-3-1-8(5-14)2-4-9/h1-4,6-7H

IXZMOLDGRAEJRY-UHFFFAOYSA-N

4-(5-chloro-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile

Linked Posts
Attached Files
8th May 2014 @ 02:38
Osm: OSM-S-211_to_OSM-S-220

(number in above picture is wrong - should be MMV669844)

Original Sources

Compound originally sourced from MMV as an enantiomerically enriched compound (MMV669844). OSM inherited data at start of Series 4 project.

Related is the synthesis of the racemate (OSM-S-208, GitHub Tag: #166)

Synthesis of 4-(5-(2-(3,4-difluorophenyl)-2-methoxyethoxy)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile (AEW 145-1)

 

Biological Data

??? - data inherited.

Metabolism ID Study for Three Triazolopyrazines

Assay Methods for Inherited Series 4 Compounds

Evaluation against Pb. Liver Schizonts

hERG Data

Related links:

Similarity of Series 4 Compounds to KAI407

Data for racemate (OSM-S-208) 

Synonyms

MMV669844

FC1=C(F)C=CC([C@@H](OC)COC2=CN=CC3=NN=C(C4=CC=C(C#N)C=C4)N32)=C1

InChI=1S/C21H15F2N5O2/c1-29-18(15-6-7-16(22)17(23)8-15)12-30-20-11-25-10-19-26-27-21(28(19)20)14-4-2-13(9-24)3-5-14/h2-8,10-11,18H,12H2,1H3

PERKBMZWWUEZNJ-UHFFFAOYSA-N

(R)-4-(5-(2-(3,4-difluorophenyl)-2-methoxyethoxy)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)benzonitrile

Attached Files
6th May 2014 @ 04:24
Osm: OSM-S-211_to_OSM-S-220

Original Sources

 

Biological Data

Single Shot Potencies for Compounds Submitted to GSK

Related links:

 

Synonyms

KAB93-5

O=C(OCCCl)N(CC1)CCC21C3=C(SC=C3)CCO2

InChI=1S/C14H18ClNO3S/c15-5-9-18-13(17)16-6-3-14(4-7-16)11-2-10-20-12(11)1-8-19-14/h2,10H,1,3-9H2

RXXGDCXYAFFODV-UHFFFAOYSA-N

2-chloroethyl 6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran]-1-carboxylate

Linked Posts
Attached Files