10334-72-2Relevant articles and documents
COMPOUND WITH AGITATION EFFECT ON PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR , AND PREPARATION METHOD AND USE THEREOF
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Page/Page column 28, (2011/06/24)
The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype δ (PPARδ), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPARδ thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.
Development of practical syntheses of potent non-nucleoside reverse transcriptase inhibitors
Kuethe, Jeffrey T.,Zhong, Yong-Li,Alam, Mahbub,Alorati, Anthony D.,Beutner, Gregory L.,Cai, Dongwei,Fleitz, Fred J.,Gibb, Andrew D.,Kassim, Amude,Linn, Kathleen,Mancheno, Danny,Marcune, Benjamin,Pye, Philip J.,Scott, Jeremy P.,Tellers, David M.,Xiang, Bangping,Yasuda, Nobuyoshi,Yin, Jingjun,Davies, Ian W.
experimental part, p. 5013 - 5023 (2009/11/30)
The development of practical and efficient syntheses of the potent non-nucleoside reverse transcriptase inhibitors 1 and 2 is described. The preparation of 1 proceeded in four synthetic steps and in 48% overall yield from 3. The long-term synthesis of 2 proceeded in nine synthetic steps and in 47% overall yield from commercially available 2,6-diflurorpyridine. The route to 2 was highlighted by the three-step synthesis of intermediate 22 and the high yielding coupling between 18 and phenol 8. The overall sequence required no chromatography and has successfully been utilized for the manufacture of 2 on large scale.