Detail of "772-79-2"

Reference

Preparation of 1,3,2-oxazaphosphacycloalkane derivatives as matrix metalloproteinase inhibitors

Preparation of 1,3,2-oxazaphosphacycloalkane derivatives as matrix metalloproteinase inhibitors. Sorensen, Morten Dahl; Blaehr, Lars Kristian Albert; Christensen, Mette Knak (Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab), Den.). PCT Int. Appl. WO 2002006293 A1 24 Jan 2002, 92 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, EE, 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, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, 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: C07F009-6584. ICS: A61K031-675. APPLICATION: WO 2001-DK464 3 Jul 2001. PRIORITY: US 2000-PV219031 18 Jul 2000. DOCUMENT TYPE: Patent CA Section: 29 (Organometallic and Organometalloidal Compounds) Section cross-reference(s): 1, 28, 63 The prepn. of 1,3,2-oxazaphosphacycloalkane derivs. [I; wherein Y = O or S; n = 1, 2, 3 or 4; X = hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R2 = H, (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl; R1 = optionally substituted alkoxyphenyl, phenoxyphenyl, phenylalkyl, naphthylalkyl, biphenyl, etc.] or a salt, hydrate or solvate thereof is described. Thus, 4-chlorophenylphosphoryl dichloride and N-(3-hydroxypropyl)glycine Et ester underwent a cyclization reaction to give Et 2-(4-chlorophenoxy)-2-oxo-1,3,2-oxazaphosphorinane-3-acetate (I; Y = O; X = CO2Et; R1 = 4-chlorophenoxy; R2 = H; n = 1). The compds. are useful in the treatment of arthritis, rheumatoid arthritis, osteoarthritis, osteopenias, osteoporosis, periodontitis, gingivitis, corneal epidermal or gastric ulceration, skin ageing, tumor metastasis, invasion or growth, multiple sclerosis, psoriasis, proliferative retinopathies, neovascular glaucoma, ocular tumors angiofibroma and hemangioma. Keywords matrix metalloproteinase inhibitor oxazaphosphacycloalkane deriv prepn Index Entries Skin, disease aging, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Blood vessel, neoplasm angiofibroma, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Gingiva gingivitis, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Blood vessel, neoplasm hemangioma, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Bone, disease osteopenia, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Periodontium periodontitis, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Alkylation Cyclization prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Eye, disease retinopathy, therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors Antiglaucoma agents Antitumor agents Antiulcer agents Arthritis Multiple sclerosis Osteoarthritis Osteoporosis Psoriasis Rheumatoid arthritis therapeutic agents; prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors 14221-01-3 51364-51-3 98327-87-8 391641-12-6 391641-13-7 391641-14-8 391641-19-3 391641-20-6 391641-23-9 391641-24-0 391641-25-1 391641-26-2 391641-27-3 391641-28-4 391641-29-5 391641-30-8 391641-31-9 391641-32-0 391641-33-1 391641-34-2 391641-35-3 391641-36-4 391641-37-5 391641-38-6 391641-39-7 391641-41-1 391641-42-2 391641-43-3 391641-44-4 391641-45-5 391641-46-6 391641-47-7 391641-48-8 391641-49-9 391641-50-2 391641-51-3 391641-52-4 391641-53-5 391641-54-6 391641-56-8 391641-15-9 391641-16-0 391641-17-1 391641-18-2 391641-21-7 391641-22-8 391641-40-0 391641-55-7 391641-57-9 391641-58-0 391641-59-1 391641-60-4 391641-61-5 391641-62-6 391641-63-7 391641-64-8 391641-65-9 391641-66-0 391641-67-1 391641-68-2 391641-69-3 391641-70-6 391641-71-7 391641-72-8 391641-73-9 391641-74-0 391641-75-1 391641-76-2 391641-77-3 391641-78-4 391641-79-5 391641-80-8 391641-81-9 391641-82-0 391641-83-1 391641-84-2 391641-85-3 391641-86-4 391641-87-5 391641-88-6 391641-89-7 391641-90-0 391641-91-1 391641-92-2 391641-93-3 391641-94-4 391641-95-5 391641-96-6 391641-97-7 391641-98-8 391641-99-9 391642-00-5 391642-01-6 391642-02-7 391642-03-8 391642-04-9 391642-05-0 391642-06-1 391642-07-2 391642-08-3 391642-09-4 391642-10-7 391642-11-8 391642-12-9 391642-13-0 391642-14-1 391642-15-2 391642-16-3 391642-17-4 391642-18-5 391642-19-6 391642-20-9 391642-21-0 391642-22-1 391642-23-2 391642-24-3 391642-25-4 391642-26-5 391642-27-6 391642-28-7 391642-29-8 391642-30-1 391642-31-2 391642-32-3 391642-33-4 391642-34-5 391642-35-6 391642-36-7 391642-37-8 391642-38-9 391642-39-0 391642-40-3 391642-41-4 391642-42-5 391642-43-6 391642-44-7 391642-45-8 391642-46-9 391642-47-0 391642-48-1 391642-49-2 391642-50-5 391642-51-6 62-53-3, reactions 98-80-6 98-88-4 105-36-2 122-01-0 156-87-6 764-11-4 772-79-2 824-72-6 2508-29-4 3497-00-5 4648-58-2 13325-10-5 33666-90-9 34909-18-7 37632-18-1 55004-22-3 68453-82-7 77918-50-4 77918-51-5 98273-58-6 118481-84-8 161518-66-7 391642-52-7 391642-53-8 391642-54-9 391642-55-0 391642-56-1 391642-57-2 391642-58-3 391642-59-4 391642-60-7 391642-61-8 391642-62-9 391642-63-0 391642-64-1 391642-65-2 391642-66-3 391642-67-4 391642-68-5 391642-69-6 391642-70-9 104125-18-0 391640-17-8 391640-18-9 391640-19-0 391640-20-3 391640-21-4 391640-22-5 391640-23-6 391640-24-7 391640-25-8 391640-26-9 391640-27-0 391640-28-1 391640-29-2 391640-30-5 391640-31-6 391640-32-7 391640-33-8 391640-34-9 391640-35-0 391640-36-1 391640-37-2 391640-38-3 391640-39-4 391640-40-7 391640-41-8 391640-42-9 391640-43-0 391640-44-1 391640-45-2 391640-46-3 391640-47-4 391640-48-5 391640-49-6 391640-50-9 391640-51-0 391640-52-1 391640-53-2 391640-54-3 391640-55-4 391640-56-5 391640-57-6 391640-58-7 391640-59-8 391640-60-1 391640-61-2 391640-62-3 391640-63-4 391640-64-5 391640-65-6 391640-66-7 391640-67-8 391640-68-9 391640-69-0 391640-70-3 391640-71-4 391640-72-5 391640-73-6 391640-74-7 391640-75-8 391640-76-9 391640-77-0 391640-78-1 391640-79-2 391640-80-5 391640-81-6 391640-82-7 391640-83-8 391640-84-9 391640-85-0 391640-86-1 391640-87-2 391640-88-3 391640-89-4 391640-90-7 391640-91-8 391640-92-9 391640-93-0 391640-94-1 391640-95-2 391640-96-3 391640-97-4 391640-98-5 391640-99-6 391641-00-2 391641-01-3 391641-02-4 391641-03-5 391641-04-6 391641-05-7 391641-06-8 391641-07-9 391641-08-0 391641-09-1 391641-10-4 391641-11-5 prepn. of 1,3,2-oxazaphosphacycloalkane derivs. as matrix metalloproteinase inhibitors

Bis(5-chloro-8-quinolyl) hydrogen phosphate as selective phosphorylating agent for nucleosides at the 5'-position

Bis(5-chloro-8-quinolyl) hydrogen phosphate as selective phosphorylating agent for nucleosides at the 5'-position. (Mitsui Toatsu Chemicals, Inc., Japan). Jpn. Kokai Tokkyo Koho JP 58135896 A2 12 Aug 1983 Showa, 5 pp. (Japanese). (Japan). CODEN: JKXXAF. CLASS: IC: C07F009-60. ICA: C07H019-10; C07H019-20. APPLICATION: JP 82-16398 5 Feb 1982. DOCUMENT TYPE: Patent CA Section: 29 (Organometallic and Organometalloidal Compounds) Section cross-reference(s): 33 The title phosphate (I; R = H) (II), useful as selective phosphorylating agent for nucleosides at 5-position, was prepd. by esterifying 4-ClC6H4OP(O)Cl (III) with 5-chloro-8-hydroxyquinoline (IV) in the presence of Et3N followed by alkali treatment of the triester (I; R = 4-ClC6H4) (V). Thus, treating 5.92 g IV with 3.68 g III and 6.21 mL Et3N in THF at 0-25° gave 76% V, which (6 g) was stirred in aq. NH4OH at room temp. to give 90% II.In this experiment, several chemicals are used like 772-79-2 and 83416-89-1 Phosphorylating 250 mg 2'-O-tetrahydropyranyluridine (VI) with 500 mg II at room temp. gave 90% VI 5'-[bis(5-chloro-8-quinolyl) phosphate]. .