On June 15, 2000, Hewawasam, Piyasena; Starrett, John E., Jr. published a patent.Related Products of 141940-37-6 The title of the patent was Preparation of 3-substituted-4-arylquinolin-2-one derivatives as calcium-activated potassium (BK) channel openers. And the patent contained the following:
The title compounds (I) [wherein R and R1 = independently H or Me; R2, R3, and R4 = independently H, halogen, NO2, or CF3; R5 = Br, Cl, or NO2; R6 = H or F; R7 = Me, CRR1OH, CHO, C:NOH, COMe, or (un)substituted aryl; m = 0-1; n = 0-6] were prepared by cyclization and further reaction of 1-[2-(acylamino)phenyl]-1-phenylmethanone derivatives For example, 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-2(1H)-quinoline (II) was synthesized in a 5-step sequence starting with acylation of 1-[2-amino-5-(trifluoromethyl)phenyl]-1′-(5-chloro-2-methoxyphenyl)methanone (preparation given) with 3-carbomethoxypropionyl chloride (82%). Subsequent cyclization (100%), dehydration (78%), demethylation (86%), and reduction of the acid yielded II. II activated the cloned BK channel mSlo expressed in Xenopus oocytes, increasing whole cell outward (K+) BK-mediated currents > 200% at 20 μM. In an in vivo erectile function test on diabetic F-344 rats, II (0.1-1 mg/kg) significantly augmented intracavernous pressure/BP responses elicited by submaximal stimulation of the cavernous nerve. As BK channel openers, I are useful in the treatment of disorders which are responsive to the opening of the potassium channels, such as ischemia, stroke, convulsions, epilepsy, asthma, irritable bowel syndrome, migraine, traumatic brain injury, spinal cord injury, sexual dysfunction, and urinary incontinence. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Related Products of 141940-37-6
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