Detail of "52449-43-1"

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Preparation of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists

Preparation of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists. Boss, Christoph; Bolli, Martin; Clozel, Martine; Fischli, Walter; Weller, Thomas (Actelion Pharmaceuticals Ltd., Switz.). PCT Int. Appl. WO 2002008200 A2 31 Jan 2002, 105 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, 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: C07D239-00. APPLICATION: WO 2001-EP7922 10 Jul 2001. PRIORITY: WO 2000-EP7006 21 Jul 2000. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Title compds. [I; R1, R2 = aryl, heteroaryl; R3 = (substituted) Ph, benzofuryl, aryl, heteroaryl; R4 = H, halo, CF3, alkyl, alkylamino, alkoxy, alkylsulfono, alkylsulfinyl, alkylthio, alkylthioalkyl, hydroxyalkyl, alkoxyalkyl, hydroxyalkyloxyalkyl, hydroxyalkylamino, alkylaminoalkyl, amino, aryl, arylthio, aryloxy, aralkyloxy, aralkyl, arylsulfinyl, heteroaryl, heteroaryloxy, heteroarylalkyloxy, heteroarylamino, heteroarylthio, heteroarylalkylthio, heteroarylalkyl, heteroarylsulfinyl, heterocyclyl, heterocyclylalkyloxy, heterocyclyloxy, heterocyclylamino, heterocyclylalkylamino, heterocyclylthio, heterocyclylalkylthio; heterocyclylalkyl, heterocyclylsulfinyl, cycloalkyl, cycloalkoxy, cycloalkylalkoxy, etc.; R5, R6 = H, alkyl; X = O, S, NH, CH2, bond; Y = O, S, NH; Z = O, S, NH, bond; Q = (CH2)n, (CH2)mCYC(CH2)p; n = 2-6; m = 1-3; p = 0-3], were prepd. Thus, NaH in THF was treated with 2-phenylethenesulfonic acid [6-(2-hydroxyethoxy)-5-p-tolylpyrimidin-4-yl]amide (prepn. given); after 1 h stirring 5-bromo-2-chloropyrimidine was added and stirring continued for 21 h at 80° to give 2-phenylethenesulfonic acid [6-[2-(5-bromopyrimidin-2-yloxy)ethoxy]-5-p-tolylpyrimidin-4-yl]amide. The latter antagonized endothelin ETA receptors with IC50 = 1.8 nM. Keywords arylethenesulfonyl pyrimidinylamide prepn endothelin receptor antagonist diabetes complication treatment arylethenesulfonyl pyrimidinylamide prepn antiinflammatory arylethenesulfonyl pyrimidinylamide prepn antimigraine arylethenesulfonyl pyrimidinylamide prepn anticancer arylethenesulfonyl pyrimidinylamide prepn antianginal arylethenesulfonyl pyrimidinylamide prepn vasospasm treatment arylethenesulfonyl pyrimidinylamide prepn ischemia treatment arylethenesulfonyl pyrimidinylamide prepn hypertension treatment arylethenesulfonyl pyrimidinylamide prepn Index Entries Endothelin receptors ETA, antagonists; prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists Endothelin receptors ETB, antagonists; prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists Anti-inflammatory agents Antianginal agents Antihypertensives Antimigraine agents Antitumor agents prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists Blood vessel, disease spasm, treatment; prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists Diabetes mellitus treatment of complications; prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists Ischemia treatment; prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists 394204-62-7 394204-63-8 394204-65-0 394204-67-2 394204-69-4 394204-70-7 394204-71-8 394204-72-9 394204-73-0 394204-74-1 394204-75-2 394204-76-3 394204-77-4 394204-78-5 394204-79-6 394204-80-9 394204-81-0 prepn. of 394204-59-2 394204-60-5 394204-61-6 394205-22-2 394205-23-3 394205-24-4 394205-25-5 394205-26-6 394205-27-7 394205-28-8 394205-29-9 394205-30-2 394205-31-3 394205-32-4 394205-33-5 394205-34-6 394205-35-7 394205-36-8 394205-37-9 394205-38-0 394205-39-1 394205-40-4 394205-41-5 394205-42-6 394205-43-7 394205-44-8 394205-45-9 394205-47-1 394205-48-2 394205-49-3 394205-51-7 394205-53-9 394205-55-1 394205-57-3 394205-60-8 394205-62-0 394205-64-2 394205-66-4 394205-68-6 394205-69-7 394205-70-0 394205-72-2 394205-75-5 394205-77-7 394205-79-9 394205-81-3 394205-83-5 394205-85-7 394205-87-9 394205-89-1 394205-91-5 394205-93-7 394205-95-9 394205-97-1 394205-99-3 394206-00-9 394206-01-0 394206-02-1 394206-04-3 394206-05-4 394206-06-5 394206-07-6 394206-08-7 394206-09-8 394206-10-1 394206-11-2 394206-12-3 394206-13-4 394206-14-5 394206-15-6 394206-16-7 394206-17-8 394206-18-9 394206-19-0 394206-20-3 394206-21-4 394206-22-5 394206-23-6 394206-24-7 394206-25-8 394206-26-9 394206-27-0 394206-28-1 394206-29-2 394206-30-5 394206-31-6 394206-32-7 394206-33-8 394206-34-9 394206-35-0 394206-36-1 394206-37-2 394206-38-3 394206-39-4 394206-40-7 394206-41-8 394206-42-9 394206-43-0 394206-44-1 394206-45-2 394206-46-3 394206-47-4 394206-48-5 394206-49-6 394206-50-9 394206-51-0 394206-52-1 394206-53-2 394206-54-3 394206-55-4 394206-56-5 394206-57-6 394206-58-7 394206-59-8 394206-60-1 394206-61-2 394206-62-3 394206-63-4 394206-64-5 394206-65-6 394206-66-7 394206-67-8 394206-68-9 394206-69-0 394206-70-3 394206-71-4 394206-72-5 394206-73-6 394206-74-7 394206-75-8 394206-76-9 394206-77-0 394206-78-1 394206-79-2 394206-80-5 394206-81-6 394206-82-7 394206-83-8 394206-84-9 394206-85-0 394206-86-1 394206-87-2 394206-88-3 394206-89-4 394206-90-7 394206-91-8 394206-92-9 394206-93-0 394206-94-1 394206-95-2 394206-96-3 394206-97-4 394206-98-5 394206-99-6 394207-00-2 394207-01-3 394207-02-4 394207-03-5 394207-04-6 394207-05-7 394207-06-8 394207-07-9 394207-08-0 394207-09-1 394207-10-4 394207-11-5 394207-12-6 394207-13-7 394207-14-8 394207-15-9 394207-16-0 394207-17-1 394207-18-2 394207-19-3 394207-20-6 394207-21-7 394207-22-8 394207-23-9 394207-24-0 394207-25-1 394207-26-2 394207-27-3 394207-28-4 394207-29-5 394207-30-8 394207-31-9 394207-32-0 394207-33-1 394207-34-2 394207-35-3 394207-36-4 394207-37-5 394207-38-6 394207-39-7 394207-40-0 394207-41-1 394207-42-2 394207-43-3 394207-44-4 394207-45-5 394207-46-6 394207-47-7 394207-48-8 394207-49-9 394207-50-2 394207-51-3 394207-52-4 394207-53-5 394207-54-6 394207-55-7 394207-56-8 394207-57-9 394207-58-0 394207-59-1 394207-60-4 394207-61-5 394207-62-6 394207-63-7 394207-64-8 394207-65-9 83-13-6 107-21-1, reactions 616-38-6 1722-12-9 4091-26-3 5638-78-8 6313-33-3 6345-27-3 14508-49-7 23786-14-3 29148-27-4 32779-36-5 34743-88-9 41841-16-1 52334-81-3 52449-43-1 57297-29-7 138588-40-6 138588-41-7 394207-66-0 394207-67-1 3974-18-3 3979-80-4 34402-92-1 146533-43-9 329923-71-9 394204-82-1 394204-83-2 394204-84-3 394204-85-4 394204-86-5 394204-87-6 394204-88-7 394204-89-8 394204-90-1 394204-91-2 394204-93-4 394204-95-6 394204-96-7 394204-98-9 394205-00-6 394205-02-8 394205-03-9 394205-05-1 394205-08-4 394205-09-5 394205-10-8 394205-12-0 394205-13-1 394205-14-2 394205-15-3 394205-16-4 394205-17-5 394205-18-6 394205-19-7 394205-20-0 394205-21-1 prepn. of arylethenesulfonic acid pyrimidinylamides as endothelin receptor antagonists

1-Aminopyrrolidine substitute and bactericidal agent composition containing it for agriculture and horticulture

1-Aminopyrrolidine substitute and bactericidal agent composition containing it for agriculture and horticulture. Yeon, Gyu Hwan; Ryu, Hun Han; Park, Chang Sik; Kim, Jin Cheol ( Korea Research Institute of Chemical Technology, S. Korea). Repub. Korean Kongkae Taeho Kongbo KR 2000009203 A 15 Feb 2000, No pp. given (Korean). (Korea, Republic Of). CODEN: KRXXA7. CLASS: ICM: C07D207-335. APPLICATION: KR 1998-29469 22 Jul 1998. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 5 1-Amino pyrrolidine substitute and a bactericidal agent compn. for agriculture and horticulture contg. it are provided which have a good bactericidal activity and wide range of antibacterial spectrum. 1-Phenylaminopyrrolidine substitute(I) and an acid addn. salt thereof having bactericidal activity on a vegetable pathogen are prepd. In a formula, R1 is H or 1-3C alkyl; R2 and R3 are independently H, halogen, 1-3C alkyl, 1-3C alkoxy, and NO2; Q is 1-phenylamino-pyrrolidine-2,5-dione substitute. For an example, 500 mL anhyd.Several substances with their cas registry numbers 52449-43-1 and 74-88-4 may be metioned in this study. DMF is mixed with 13.1g of sodium hydride at 0° and agitated with 50 g Me 2-(4-chlorophenyl)acetate. The reactant is agitated with 42.3 g Me iodide, added with 1,000 mL ice water, and extd. twice with 200 mL dichloromethane. An org. layer is dried with anhyd. sodium sulfate, concd. and purified using a column chromatog. to 50.0 g Me 2-(4-chlorophenyl)propanoate. The product shows good bactericidal activity on Pyricularia, Rhizoctonia solani, Bltrytis cinerea, Phutophthora infestans. .