On August 4, 2016, Dejesus, Reynalda K.; Fu, Qinghong; Jiang, Jinlong; Tang, Haifeng published a patent.Synthetic Route of 1198284-94-4 The title of the patent was Preparation of novel spirocyclic compounds as inhibitors of the renal outer medullary potassium channel. And the patent contained the following:
The title compounds I [R1 = H, halo, OH, alky, alkoxy; R2 = H, alkyl; R3 = H, or alkyl optionally substituted with OH, OMe or 1-3 halo; or R3 and R4 are joined together to form CH2CH2; R4 = H, or alkyl optionally substituted with OH, OMe or 1-3 halo; n = 1-2; m = 1-2, wherein when m = 2, X3 = CH2; R5 = H, halo, cycloalkyl or alkyl; X1 = C(O), CH2; X2 = O, CH2; X3 = C(O), CH2, wherein when X3 = CH2, m = 2;X4 = C(O), SO2; Z = II or III (Y1-Y4 = (independently) CR9 or N; provided that at most two of Y1-Y4 are N; R9 = (independently) H, halo, alkoxy or alkyl optionally substituted with 1-3 halo; R10 = H, halo, alkyl optionally substituted with 1-3 halo; R11 = H, alkyl optionally substituted with 1-3 halo; R12 = H or alkyl)] which are inhibitors of the ROMK (Kir1.1) channel, were prepared For example, microwaving a solution of (1R,3r,5S)-1′-(2-methyl-3-oxocyclopent-1-en-1-yl)-8-azaspiro[bicyclo[3.2.1]octane-3,3′- pyrrolidin]-2′-one and (R)-4-methyl-5-(oxiran-2-yl)isobenzofuran- 1(3H)-one in EtOH at 145°C for 4.5 h afforded IV. Exemplified compounds I were tested in the thallium flux assay (data given). The compounds I may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions comprising I, alone or in combination with other therapeutic agent, are disclosed. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Synthetic Route of 1198284-94-4
The Article related to spirocyclic compound preparation renal outer medullary potassium channel inhibitor, romk inhibitor diuretic natriuretic cardiovascular antihypertensive spirocyclic compound preparation, heart failure chronic kidney disease treatment spirocyclic compound preparation, excessive salt water retention treatment spirocyclic compound preparation and other aspects.Synthetic Route of 1198284-94-4
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