Synthesis of a Bicyclic Azetidine with in Vivo Antimalarial Activity Enabled by Stereospecific, Directed C(sp3)-H Arylation

Journal of the American Chemical Society

Volumn 139, Issue 32, 2017, Pages 11300-11306

  Maetani, Micah ^a,b   Zoller, Jochen ^a,b   Melillo, Bruno ^a,b   Verho, Oscar ^a,b   Kato, Nobutaka ^b   Pu, Jun ^b   Comer, Eamon ^b   Schreiber, Stuart L ^a,b,c  

^a HARVARD UNIVERSITY   (United States)

^b BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^c HOWARD HUGHES MEDICAL INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AROMATIC COMPOUNDS; LIFE CYCLE;

ANTIMALARIAL ACTIVITY; ANTIMALARIAL COMPOUNDS; ANTIMALARIAL DRUG; COST CONSTRAINTS; EFFICIENT SYNTHESIS; NEW THERAPEUTIC AGENT; PLASMODIUM FALCIPARUM; SYNTHETIC ROUTES;

CHEMICAL REACTIONS;

ANTIMALARIAL AGENT; AZETIDINE DERIVATIVE; BRD 3914; CHLOROQUINE; PALLADIUM; UNCLASSIFIED DRUG; BRIDGED BICYCLO COMPOUNDS;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; ARTICLE; ARYLATION; CATALYSIS; CONTROLLED STUDY; DRUG SYNTHESIS; HEK293 CELL LINE; HEP-G2 CELL LINE; HUMAN; HUMAN CELL; IN VIVO STUDY; MALARIA FALCIPARUM; MOUSE; NONHUMAN; PLASMODIUM FALCIPARUM; SINGLE DRUG DOSE; STEREOSPECIFICITY; ANIMAL; CHEMISTRY; DISEASE MODEL; DRUG EFFECT; NONOBESE DIABETIC MOUSE; SCID MOUSE; STEREOISOMERISM; SYNTHESIS;

ANIMALS; ANTIMALARIALS; AZETIDINES; BRIDGED BICYCLO COMPOUNDS; CATALYSIS; DISEASE MODELS, ANIMAL; HEP G2 CELLS; HUMANS; MALARIA, FALCIPARUM; MICE, INBRED NOD; MICE, SCID; PALLADIUM; PLASMODIUM FALCIPARUM; STEREOISOMERISM;

EID: 85027412300     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/jacs.7b06994     Document Type: Article

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