Reference

Carbon-14 labeling of selective H3 receptor antagonists

All Rights Reserved. Carbon-14 labeling of selective H3 receptor antagonists. Johansen, Steen K. (Isotope Chemistry, Maaloev DK-2760, Den.). 659-28-9 is the cas registry number. This chemical is also mentioned in this article. Journal of Labelled Compounds & Radiopharmaceuticals, 48(14), 1025-1029 (English) 2005 John Wiley & Sons Ltd. CODEN: JLCRD4. ISSN: 0362-4803. DOCUMENT TYPE: Journal CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 25 The fast and efficient carbon-14 labeling of the three potent H3 antagonists NNC 38-1202 [i.e., (2S)-1-[(2E)-1-oxo-3-[4-(trifluoromethyl)phenyl]-2-propenyl-2-14C]-2-(1-p yrrolidinylmethyl)pyrrolidine], NNC 38-1384 [i.e., (2S)-1-[(2E)-1-oxo-3-[4-(trifluoromethyl)phenyl]-2-propenyl-2-14C]-2-(1-p iperidinylmethyl)pyrrolidine] and NNC 38-1401 [i.e., (2S)-1-[(2E)-1-oxo-3-[4-(trifluoromethoxy)phenyl]-2-propenyl-2-14C]-2-(1 -piperidinylmethyl)pyrrolidine] is reported. The two-step synthetic sequence, which included a Knoevenagel reaction, provided the carbon-14-labeled compds. in 38-55% overall yield starting from [2-14C]malonic acid. The compds. were all obtained in high radiochem. purity (>99%) and with high specific activity (55.8 mCi/mmol). .

Preparation of 2-alkenyl-5-(1,2,4-triazol-1-yl)methyl-1,3-oxathiolane derivatives as fungicides for humans and animals

Preparation of 2-alkenyl-5-(1,2,4-triazol-1-yl)methyl-1,3-oxathiolane derivatives as fungicides for humans and animals. Oida, Sadao; Tajima, Kazu; Yasuda, Hiroshi (Sankyo Co, Japan). Jpn. Kokai Tokkyo Koho JP 08333367 A2 17 Dec 1996 Heisei, 17 pp. (Japanese). (Japan). CODEN: JKXXAF. CLASS: ICM: C07D411-06. ICS: C07D411-14; A61K031-41; A61K031-44. APPLICATION: JP 1995-143410 9 Jun 1995. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 The title compds. [I; R1 = Ph optionally substituted by 1-3 substituents selected from halo and CF3 ; Ar2 = Ph, pyridyl, furyl, or thienyl each optionally substituted by 1-3 substituents selected from lower (halo)alkyl, lower (halo)alkoxy, halo, NO2, cyano, S(O)mR7, and NHCOR8; wherein R7 = lower (halo)alkyl and m = 0,1,2; R8 = lower alkyl; R1 = lower alkyl; R2 = H, lower alkyl; R3 - R6 = H, lower alkyl optionally substituted by halo, OH, lower (halo)alkoxy, lower alkanoyloxy, S(O)mR7, and NHCOR8; p = 0,1] are prepd. Thus, (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-bu tanol and trans-4-(methylsulfonyl)cinnamaldehyde were stirred in the presence of p-MeC6H4SO3H.H2O and mol. sieve 4A at room temp. for 30 min, followed by treatment with trimethylsilyl triflate under ice-cooling, and after 10 min, the resulting mixt. was treated with aq. NaHCO3 and extd. with EtOAc to give 41% the title compd. (II). The compds. 659-28-9 is just another one chemical used in this study. II in vivo were more potent against infection of mice with Candida albicans ketoconazole (no details data given). .