Detail of "410545-86-7"

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Process for the preparation of a Na salt of a 5-(dioxidothiazinanyl)naphthyridine-7-carboxamide HIV integrase inhibitor

Process for the preparation of a Na salt of a 5-(dioxidothiazinanyl)naphthyridine-7-carboxamide HIV integrase inhibitor. Anthony, Neville J.; Xu, Wei; Lepore, John V.Several substances are used for example 410545-86-7 which is its cas registry number.; Mahajan, Amar J. (Merck & Co., Inc., USA). PCT Int. Appl. WO 2003016315 A1 27 Feb 2003, 40 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, 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, NO, NZ, OM, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; 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: C07D487-06. ICS: A61K031-4375; A61P031-18. APPLICATION: WO 2002-US25675 13 Aug 2002. PRIORITY: US 2001-PV313373 17 Aug 2001. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 The cryst. sodium salt I·Na was prepd. as an HIV integrase inhibitor for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS (no data). 410545-86-7 is just another one chemical used in this study. I·Na exhibited superior oral bioavailability and improved pharmacokinetics (e.g., improved Cmax and AUC) in rats and dogs relative to amorphous and cryst. I (no data). For example, 5-bromo-8-(p-toluenesulfonyloxy)-1,6-naphthyridine-7-carboxylic acid Me ester was coupled with 1,4-butane sultam (prepn. of starting materials given) in the presence of Cu2O and 2,2'-bipyridyl in DMF (78%). Deprotection of the alc. with NaOMe in MeOH (97%), followed by amidation with 4-fluorobenzylamine in EtOH gave I·EtOH (94%). The cryst. Na salt of 5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naph thyridine-7-carboxamide (I·Na) was formed by treating the monoethonalate with 5M NaOH in a mixt. of EtOH and H2O. I·Na was analyzed by differential scanning calorimetry at a heating rate of 10°C/min in an open cup under flowing nitrogen and was found to have a DSC curve exhibiting an endotherm with a peak temp. of about 348° and an assocd. heat of fusion of about 45 J/gm followed by an exotherm with a peak temp. of about 352° and an assocd. heat of fusion of about 45 J/gm. The X-ray powder diffraction pattern of the Na salt was also generated. ..

Process for the preparation of a Na salt of a 5-(dioxidothiazinanyl)naphthyridine-7-carboxamide HIV integrase inhibitor

Process for the preparation of a Na salt of a 5-(dioxidothiazinanyl)naphthyridine-7-carboxamide HIV integrase inhibitor. Anthony, Neville J.; Xu, Wei; Lepore, John V.Several substances are used for example 410545-86-7 which is its cas registry number.; Mahajan, Amar J. (Merck & Co., Inc., USA). PCT Int. Appl. WO 2003016315 A1 27 Feb 2003, 40 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, 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, NO, NZ, OM, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; 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: C07D487-06. ICS: A61K031-4375; A61P031-18. APPLICATION: WO 2002-US25675 13 Aug 2002. PRIORITY: US 2001-PV313373 17 Aug 2001. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 The cryst. sodium salt I·Na was prepd. as an HIV integrase inhibitor for preventing or treating HIV infection, for delaying the onset of AIDS, and for treating AIDS (no data). 410545-86-7 is just another one chemical used in this study. I·Na exhibited superior oral bioavailability and improved pharmacokinetics (e.g., improved Cmax and AUC) in rats and dogs relative to amorphous and cryst. I (no data). For example, 5-bromo-8-(p-toluenesulfonyloxy)-1,6-naphthyridine-7-carboxylic acid Me ester was coupled with 1,4-butane sultam (prepn. of starting materials given) in the presence of Cu2O and 2,2'-bipyridyl in DMF (78%). Deprotection of the alc. with NaOMe in MeOH (97%), followed by amidation with 4-fluorobenzylamine in EtOH gave I·EtOH (94%). The cryst. Na salt of 5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naph thyridine-7-carboxamide (I·Na) was formed by treating the monoethonalate with 5M NaOH in a mixt. of EtOH and H2O. I·Na was analyzed by differential scanning calorimetry at a heating rate of 10°C/min in an open cup under flowing nitrogen and was found to have a DSC curve exhibiting an endotherm with a peak temp. of about 348° and an assocd. heat of fusion of about 45 J/gm followed by an exotherm with a peak temp. of about 352° and an assocd. heat of fusion of about 45 J/gm. The X-ray powder diffraction pattern of the Na salt was also generated. ..