Reference

Preparation of (+)-2-(2,4-difluorophenyl)-1-[3-[(E)-4-(2,2,3,3,-tetrafluoropropoxy)styryl]- 1H-1,2,4-triazol-1-yl]-3-(1H-1,2,4-triazol-1-yl)propan-2-ol as medical fungicide

Preparation of (+)-2-(2,4-difluorophenyl)-1-[3-[(E)-4-(2,2,3,3,-tetrafluoropropoxy)styryl]- 1H-1,2,4-triazol-1-yl]-3-(1H-1,2,4-triazol-1-yl)propan-2-ol as medical fungicide. Murakami, Kimihiro; Mochizuki, Hidenori (Imperial Chemical Industries PLC; Mochida Pharmaceutical Co., Ltd., UK). Eur. Pat. Appl. EP 472392 A2 26 Feb 1992, 28 pp. DESIGNATED STATES: R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE. (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07D249-08. ICS: C07D303-12; C07D405-06; A61K031-41. APPLICATION: EP 91-307624 19 Aug 1991. PRIORITY: JP 90-223894 24 Aug 1990. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 The title compd. (I) was prepd. as a medical fungicide. Thus 4-(2,2,3,3-tetrafluoropropoxy)benzaldehyde (prepn. from 2,2,3,3-tetrafluoropropanol and 4-chlorobenzonitrile given) was olefinated by (EtO)2P(O)CH2CO2Et and the product formed was hydrolyzed to the acid then amidated to give (E)-4-(2,2,3,3-tetrafluoropropoxy)cinnamamide. This was treated with Me3OBF4 then cyclized with H2NNHCHO to give 3-[(E)-4-(2,2,3,3-tetrafluoropropoxy)styryl-1H-1,2,4-triazole. This was heated at 90° for 1 h with (+)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)-2,3-epoxypropane (prepn. given) and K2CO3 in DMF to give I. 1774-47-6 and 288-88-0 which are cas registry numbers of substances are two of reagents here. I had ED50 of 19.7 mg/kg in vivo in mice against Cryptococcus neoformans compared with 43.5 and >100 mg/kg for racemic I and fluconazole resp. Formulations contg. I are given. .

Sulfur ylide complexes of palladium

Sulfur ylide complexes of palladium. Preparation of organometallic compounds by the phase transfer catalysis technique. Lin, Ivan J. B.; Lai, Hanse Y. C.; Wu, Shu C.; Hwan, Luchen (Dep. Chem., Fu Jen Cathol. Univ., Taipei 24205, Taiwan). J. Organomet. Chem., 306(1), C24-C26 (English) 1986. CODEN: JORCAI. ISSN: 0022-328X. DOCUMENT TYPE: Journal CA Section: 29 (Organometallic and Organometalloidal Compounds) Reactions of [S(O)Me3]I in aq. 1774-47-6 and 107246-96-8 which are cas registry numbers of chemicals are mentioned. NaOH-CHCl3 with Pd(PPh3)2Cl2 in the presence of Bu4NI produced the cationic and neutral bidentate sulfur ylide complexes I and II, resp., in >60% yields. II converted to I in CHCl3 at ambient temp. Without the phase transfer catalyst, no ylide complexes were formed. I, II, and cis-[Pd(PPh3)2[CH2S(O)Me2]2]I2 were also prepd. in ~10% yields by reaction of H2C:S(O)Me2 with Pd(PPh3)2Cl2 in THF under an inert atm. The advantages of the phase transfer technique are discussed. .