Detail of "569351-62-8"

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A preparation of spirolactone derivatives, useful as NPY5 antagonists

A preparation of spirolactone derivatives, useful as NPY5 antagonists. Volante, Ralph P.; Weissman, Steven A.; Iida, Takehiko; Yamamoto, Yuhei; Sato, Hiroki; Maeda, Kenji; Sawada, Naotaka; Mase, Toshiaki ( Merck & Co., Inc.; Banyu Pharmaceutical Co., Ltd., USA). PCT Int. Appl. WO 2004104009 A1 2 Dec 2004, 47 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D491-10. ICS: A61K031-4355; A61P009-00; A61P025-00; A61P003-00; C07D307-00; C07D221-00. APPLICATION: WO 2004-US15051 14 May 2004. PRIORITY: US 2003-PV471680 19 May 2003. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 45 The invention relates to a prepn. of spirolactone derivs. of formula I [wherein: T, U, V, and W are independently selected from N or (un)substituted methine; at least two of T, U, V, and W are methine], useful as NPY5 antagonists (no biol. data). For instance, spirolactone deriv. II·HCl was prepd. via intramol. lactonization of pyridine-3-(1-hydroxy-cyclohex-1-yl)-4-carboxylic acid deriv. III and subsequent sepn. 569351-62-8 is the cas registry number of certain chemical which is used as reagents here. of diastereomers. .

Preparation of (hetero)aryl-fused spirolactones from (hetero)arylcarboxamides and cyclohexanones

Preparation of (hetero)aryl-fused spirolactones from (hetero)arylcarboxamides and cyclohexanones. Volante, Ralph P.; Tschaen, David M.; Weissman, Steven A.; Heileman, Matthew; Mase, Toshiaki; Iida, Takehiko; Maeda, Kenji; Wada, Toshihiro; Sato, Hiroki; Asakawa, Kenichi (Merck & Co., Inc.; Banyu Pharmaceutical Co., Ltd., USA). PCT Int. Appl. WO 2004037170 A2 6 May 2004, 64 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2.In this article, certain chemicals are used. One of their cas registry numbers is 569351-62-8 CLASS: ICM: A61K. APPLICATION: WO 2003-US32393 14 Oct 2003. PRIORITY: US 2002-PV419464 18 Oct 2002. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Title compds. [I; T, U, V, W = N, (substituted) CH; 32 of T, U, V, W = CH], were prepd. by combining a strong base with amides (II; R5, R6 = H, alkyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl; T, U, V, W as above) in an aprotic solvent to form a soln., reacting cyclohexanones [III; R1 = (protected) CO2H, cyano, CH2OH, aryl, ester, ketal] with the soln., converting R1 to CO2H if needed, and adding an acid. Thus, N-phenylisonicotinamide and LiBr in THF at -65° were treated with BuLi followed by aging at <-55° for 1-7 h and addn. to a soln. of Et 4-oxocyclohexanecarboxylate in THF at <-60°, aging for 1 h, and quenching with H2O to give an aq. soln. of diacid. Ths was treated with H2SO4 to pH 2-3 followed by aging for 1-4 h at 30-70° and extn. with THF to give a suspension of 1'-oxospiro[cyclohexane-1,3'-furo[3,4-c]pyridine]-4-carboxylic acid. This was aged in 3.3 M HCl/EtOAc at 40-60° for 24-48 h to give the trans-acid. .