Regular Issue

Vol. 26, No. 1, 1987

37 data found. 31 - 37 listedFirst Previous
Paper | Regular issue | Vol 26, No. 1, 1987, pp. 163 - 173
Published online:
DOI: 10.3987/R-1987-01-0163
Reaction of Amidoximes with α-Chloroacid Chlorides: Novel Synthesis of 1,2,4-Oxadiazin-5-ones

Ahmad Q. Hussein

*Chemistry Department, Faculty of Science, University of Jordan, Amman 11942, Jordan


The reaction of amidoximes with α-chloroacid chlorides gives under thermal reaction conditions 5-(1-chloroalky1)-l,2,4-oxadiazoles. In presence of a strong base, the reaction follows a different path leading to the formation of 4H-1,2,4-oxadiazin-5(6H)-ones (4). This latter transformation, involving 0 → N acyl migration, constitutes a new convenient route to compounds 4.

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Paper | Regular issue | Vol 26, No. 1, 1987, pp. 175 - 179
Published online:
DOI: 10.3987/R-1987-01-0175
A New Synthesis of Pyrimido[4,5-b][1,5]benzodiazepin-2-one and -2-thione Derivatives

Kaname Takagi, Hikari Morita, Tomoji Aotsuka, and Yoshihisa Okamoto

*Central Research Laboratories, Zeria Pharmaceutical Co.,, Oshikiri, Konan-machi, Oato-gun, Saitama 360-0111, Japan


Derivatives of pyrimido[4,5-b][1,5]benzodiazepin-2- one and -2-thione were synthesized by intramolecular cyclization of N-(3-cyano-1H-1 ,5-benzodiazepin-4-y1)-N’-alkylureas and -N’-phenylthiourea which were obtained by reactions of 4-amino-1H-1,5-benzodiazepine-3-carbonltrile with alkyl isocyanates and phenyl isothiocyanate, respectively.

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Paper | Regular issue | Vol 26, No. 1, 1987, pp. 181 - 190
Published online:
DOI: 10.3987/R-1987-01-0181
Reaction of Benzamiode Oxime Derivatives with Chlorocarbonylsulfenyl Chloride

Etsuko Kawashima, Yuko Ando, Toyozo Takada, and Katsumi Tabei

*Tokyo University of Pharmacy and Life Science, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan


Benzamide oxime derivatives (1) were reacted with chlorocarbonylsulfenyl chloride (2) in the presence of a base as a catalyst to afford 3-aryl-4,5-dihydro-1,2,4 -thiadiazol-5-one (3). 3-aryl-4,5-dihydro-1,2,4-oxadiazol-5-one (4) and di(benzamide) 0,0’-carboxime (5) derivatives in moderate yields. The reaction of N-ethyl-p-toluamide oxime (7) with 2 gave 4-ethyl-4,5-dihydro-3-(p-tolyl)-1,2,4-thiadiazol-5-one (8) and 4-ethyl-4,5-dihydro-3-(p-tolyl)-1,2,4-oxadiazol-5-one (9).

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Paper | Regular issue | Vol 26, No. 1, 1987, pp. 191 - 197
Published online:
DOI: 10.3987/R-1987-01-0191
Reaction of Spiro[piperidine-4,2’-(1’,2’,3’,4’-tetrahydroquinazolin)]-4’-ones with Acetic Anhydride

Masatoshi Yamato, Yasuo Takeuchi and Yuji Ikeda

*Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-naka, Okayama 700-8530, Japan


The tetrahydro derivative (5a) and its aza derivative (5b) of antitumor active amsacrine were prepared. The key synthetic intermediate (3a) was simply prepared by rearrangement of spiro-compound (2a) by heating with acetic anhydride and pyridine. On the other hand, another key intermediate (3b) was obtained only during moderated reaction conditions, and the ring opening products (6b,b’ and 8b,b’) were obtained under the usal conditions.

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Paper | Regular issue | Vol 26, No. 1, 1987, pp. 199 - 204
Published online:
DOI: 10.3987/R-1987-01-0199
A Novel Synthesis of Pyrrolo[2,1,5-de]quinolizinones (Cycl[3.3.2]azinones)

Yasuyoshi Miki,* Hisashi Kinoshita, Toshihiko Yoshimaru, Shoji Takemura, and Masazumi Ikeda

*Faculty of Pharmaceutical Sciences, Kinki University, 3-4-1, Kowakae, Higashi-Osaka 577-8502, Japan


3H-Pyrrolo[2,1,5-de]quinolizin-3-ones and a 5H-pyrrolo-[2,1,5-de]quinolizin-5-one were synthesized by the intramolecular aldol condensation of the appropriate 3,5-diacylindolizines.

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Review | Regular issue | Vol 26, No. 1, 1987, pp. 205 - 238
Published online:
DOI: 10.3987/R-1987-01-0205
Chemistry of α-Cyanothioacetamide

Bahia Y. Riad, Abdallah M. Negm, Sedek E. Abdou, and Hamed A. Daboun

*Department of Chemistry, Faculty of Science, University of Cairo, Giza, Egypt


The methods of preparation, chemical properties and utility of a-cyanothioacetamide in the synthesis of sulphur and nitrogen heterocyclic compounds are reviewed.

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Review | Regular issue | Vol 26, No. 1, 1987, pp. 239 - 273
Published online:
DOI: 10.3987/R-1987-01-0239
Recent Advances in the Synthesis of Phenothiazines

Sayeed Saraf, Fatima Al-Omran, and Balkis Al-Saleh

*Department of Chemistry, Faculty of Science, University of Kuwait, Safat 13060, P.O. Box 5969, Kuwait


This paper reviews the most recent methods for the synthesis of phenothiazine derivatives.

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