The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-Butan-2-ol( cas:4221-99-2 ) is researched.Category: tetrahydrofurans.Larsen, Jens; Lambert, Maja; Pettersson, Henrik; Vifian, Thomas; Larsen, Mogens; Ollerstam, Anna; Hegardt, Pontus; Eskilsson, Cecilia; Laursen, Steen; Soehoel, Anders; Skak-Nielsen, Tine; Hansen, Lene M.; Knudsen, Nina Oe.; Eirefelt, Stefan; Soerensen, Morten D.; Stilou, Tatiana G.; Nielsen, Simon F. published the article 《Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel “”Dual-Soft”” PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis》 about this compound( cas:4221-99-2 ) in Journal of Medicinal Chemistry. Keywords: isobutyl methoxyoxo isobenzofuranyl triazolopyridinyl cyclopropanecarboxylate LEO 39652 preparation; PDE4 inhibitor topical stability atopic dermatitis LEO 39652 metabolism. Let’s learn more about this compound (cas:4221-99-2).
We describe the design of a novel PDE4 scaffold and the exploration of the dual-soft concept to reduce systemic side effects via rapid elimination: introducing ester functionalities that can be inactivated in blood as well as by the liver (dual-soft) while being stable in human skin. Compound 40 was selected as a clin. candidate as it was potent and rapidly degraded by blood and liver to inactive metabolites and because in preclin. studies it showed high exposure at the target organ: the skin. Preclin. and clin. data are presented confirming the value of the dual-soft concept in reducing systemic exposure.
From this literature《Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel “”Dual-Soft”” PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis》,we know some information about this compound(4221-99-2)Category: tetrahydrofurans, but this is not all information, there are many literatures related to this compound(4221-99-2).
Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem