On March 29, 2012, Bartolozzi, Alessandra; Bosanac, Todd; Chen, Zhidong; De Lombaert, Stephane; Huber, John D.; Liu, Weimin; Lo, Ho Yin; Loke, Pui Leng; Riether, Doris; Tye, Heather; Wu, Lifen; Zindell, Renee M. published a patent.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of oxadiazole inhibitors of leukotriene production. And the patent contained the following:
The title compounds I [R1, R2 = H, alkyl, carboxyxlice (with the proviso that both R1 and R2 are not hydrogen); R3 = (un)substituted 5-11 membered heteroaryl ring containing 1-3 heteroatoms selected from N, O and S; R4 = H, halo, alkyl, nitrile; R5 = (un)substituted alkyl, C3-10 carbocycle, 5-11 membered heterocycle, etc.], useful in treating a leukotriene-mediated disorders, were prepared Thus, reacting compound II (preparation given) with the pyrimidine derivative III afforded the title compound IV. Biol. testing showed that compounds I are effective inhibitors of 5-lipoxygenase activating protein (FLAP) and thus inhibit leukotriene production (IC50 values were given). The invention also relates to pharmaceutical compositions comprising compounds I, methods of I in the treatment of various diseases and disorders, processes for preparing I and intermediates useful in these processes. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid
The Article related to oxadiazole preparation leukotriene production ltb4 inhibitor, lipoxygenase activating protein flap inhibitor oxadiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics