Abstract:
Prostaglandin analogues and their intermediates (I; R1 and R2 are different, H or hydroxyl group, R3 = C1-5 alkyl, R4 = C1-5 alkyl, R5 = tetrahydropyranyl of H,U = (CH2)m, m = 0-5, R6 and R7 are same or not, H or C1-5 alkyl group, V = C1-5 alkyl, W =C1-5 alkyl, X = (CH2) m, m = 0-5). The compds, had strong antiprostaglandin activity. Thus, compd. II was reacted with hydrated metal complex to give I.
Abstract:
Title compds. I(R1,R2 = O, H, HO; R3 = H, C1-8 alip. or Cycloalip. group, C7-9 aralip., substituted ammonium ion; R4 = C1-10 alip. hydrocarbon, C3-7 cycloalip. hydrocarbon; R5 = H, alkyl, alkenyl, alkynyl; R6 = H, alkyl; A = trans -CH=CH- or -CH2-CH2-), useful hypertensives, were prepd. by reacting compd. II with acylating agent contg. C2-11 carboxylic group. Thus, 9-keto-15α--hydroxy-16,16-dimethyl-18- oxa -prosta-2,13-dienic acid methyl ester was dissolved in anhydrous dimethoxy ethane and added to a mixt. of dimethoxy ethane, pyridine and acetyl chloride to give 9-keto-15α-acetoxy-16,16-dimethyl-18-oxa-prosta-2,13-dienic acid methyl ester.
AND SALTS THEREOF WITH PHYSIOLOGICALLY TOLERABLE ACIDS, WHEREIN R1 HYDROGEN, ALKYL, PHENYL, OR HALO-, ALKYL-, OR ALKOXY-SUBSTITUTED PHENYL; R2, R3, AND R4 MAY BE THE SAME OR DIFFERENT AND ARE HYDROGEN, ALKYL, ALKOXY, OR HALOGEN; AND R5 IS ALKYL OR PHENYL.
Abstract:
Analgesic composition containing, as an essential active ingredient, a 1-vinylcarbonyl-piperazine compound of the formula
OR A SALT THEREOF WITH PHYSIOLOGICALLY TOLERABLE ACID, WHEREIN R1 is hydrogen, alkyl, phenyl, or halo-, alkyl-, or alkoxysubstituted phenyl; R2, R3, and R4 may be the same or different and are hydrogen, alkyl, alkoxy, or halogen; and R5 is alkyl or phenyl.
Abstract:
Isoquinolines I(R1 = amino group -N(R4)(R5); R4, R5 = alky1 and make 5-8 membered cycle with N; R2 = halogen, OH, nitro, amino, substituted amino, mono- or di-substituted pheny1, pyridy1 or thieny1; R3 = H, OH, halogen, C1-6 alky1, alkoxy, NO2, amino, ethylenedioxy; m = 1,2), exhibiting effective activities for melancholia, were prepd. by reacting compds. II (X = H, carboxy1; Y = cl, Br) with amines (III). Thus, 3-chloro-1-pheny1-isoquinoline-4-carboxylic acid was heated to 150oC in N-methy1-piperazine and maintained for 6 hr to give 3-N-methy1piperazino-1-pheny1-isoquinoline.
Abstract:
Title compds.(I; R1 = H, C1-10 hydrocarbon, ammonium ion; R2 = C1-6 aliphatic hydrocarbon) were prepd. by the hydrolysis of IV(R3 = protecting group; Z = CH2 or -C(CH3)2 group) obtained from the reaction of II and III (R4 = C1-4 alkyl or phenyl). Thus, 111.2 g 3-carbomethoxy-2-propenyl-2-triphenyl-phosphonium bromide and 71.6 g methyl-γ-bromo-crotonate were stirred at 26oC for 1.5 hr to give I.
Abstract:
Prostanoic acid [I; u= (CH2)m, m = 0-5, - R3CCR4-, (R3 = / ≠ R4 = H, C1-C5 alkyl, but when X is (CH2)1-3, R3,R4 ≠ H at the same time), V= single bond, O, W = R5CR6 (R5 = / ≠ R6 = 0), C1-C5 alkyl) and its acid salts useful as anticonvulsive, were prepd. by retro-Dieckmann condensation of II to give III, followed by alkali safonification of III, decarboxylating, and then isolating ethers from III.