- Synthesis, crystal structure, spectral and DFT studies of potent isatin derived metal complexes
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The isatin-core in compounds offers exciting perspectives in medicinal and pharmacological research. The present study reports the successful development of new isatin-core transition metal based anti-bacterial complexes via conventional refluxing method.
- Sumrra, Sajjad Hussain,Atif, Aftab Hussain,Zafar, Muhammad Naveed,Khalid, Muhammad,Tahir, Muhammad Nawaz,Nazar, Muhammad Faizan,Nadeem, Muhammad Arif,Braga, Ataualpa A.C.
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- Synthesis of quinazolindionyl amino acid and hydrazone derivatives as possible antitumour agents
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A series of 1-ethyl-2,4-dioxo-(1H,3H)-quinazolin-3-yl amino acid and hydrazone derivatives were synthesized and tested for their antitumor activity. The alcohol and acid derivatives of quinazolindione were conjugated with the amino acid derivatives at N-3 site via ester or amide bonds by carbodiimide and azide methods. The carbodiimide-mediated amide and esterification steps were performed in the presence of HOBt or DMAP respectively otherwise the side-products N-acyl urea derivatives are formed, instead of the desired derivatives. Nine compounds exhibited encouraging antitumor activity against human liver carcinoma cell line (HepG2).
- Aboelmagd,Salem, Ezzeldin M.S.,Ali, Ibrahim A.I.,Gomaa, Mohamed S.
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- Ketoserin intermediate and preparation method of ketoserin
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The invention discloses a preparation method of a ketoserin intermediate 2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone and a preparation method of ketoserin, and the reaction equation of the preparation method of the ketoserin intermediate 2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone is shown in the specification: in the reaction, sodium carbonate and acetonitrile are used, no catalyst is added, inorganic salt is removed through hot filtration after the reaction, filtrate is evaporated to dryness, acetonitrile is recycled, and an intermediate 04, namely the ketoserin intermediate2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone, is obtained. The method is simple and convenient to operate, lower in cost, better in product character and more beneficial to synthesis of a finalproduct.
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Paragraph 0045-0046; 0048-0050
(2021/01/15)
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- Reinvestigation of the synthesis of ketanserin (5) and its hydrochloride salt (5.HCl) via 3-(2-chloroethyl)-2,4-(1H,3H)-quinazolinedione (2) or dihydro-5H-oxazole(2,3-b)quinazolin-5-one (1)
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The synthesis of ketanserin (5) and its hydrochloride salt (5.HCl) using respectively equimolar amounts of 3-(2-chloroethyl)-2,4-(1H,3H)-quinazolinedione (2) with 4-(parafluorobenzoyl)piperidine (3) and dihydro-5H-oxazole(2,3-b) quinazolin-5-one (1) with hydrochloride salt of 4-(parafluorobenzoyl)piperidine (3.HCl) is reinvestigated. The one-pot reaction of ethyl-2-aminobenzoate with ethyl chloroformate and ethanol amine has afforded 3-(2-chloroethyl)-2,4-(1H,3H) -quinazolinedione (2) (86%) that was then refluxed with 4-(parafluorobenzoyl) piperidine (3) in ethyl methyl ketone in the presence of sodium carbonate to obtain free base of ketanserin (87%). In another attempt, a very pure hydrochloride salt of ketanserin (5.HCl) was synthesized using equimolar amounts of dihydro-5H-oxazole(2,3-b)quinazolin-5-one (1) and hydrochloride salt of 4-(parafluorobenzoyl)piperidine (3.HCl) by a solvent-less fusion method. Thus, under optimized conditions, 180°C and a reaction time of 30 min, the powder mixture was transformed into glassy crystals that were initially readily soluble in chloroform but were transformed afterwards over time (2 h) to white precipitates (5.HCl) suspended in chloroform with a yield of 72%.
- Fakhraian, Hossein,Heydary, Mehdi
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p. 151 - 156
(2014/02/14)
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- 4-Hydroxy-2-quinolones 173. 1-R-3-(2-diethylamino- ethyl)-1H-quinazoline- 2,4-dione hydrochlorides as potential local anesthetic agents
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Different variants of the preparation and procedures in the synthesis of a series of 1-R-3-(2-dialkyl-aminoethyl)-1H-quinazoline-2,4-dione hydrochlorides having a structural similarity to the 4-hydroxy-2-quinolinone anesthetic chinoxicaine are discussed. A comparative analysis of the biological properties of the synthesized compounds and the known local anesthetics chinoxicaine and lidocaine is reported.
- Ukrainets,Kravtsova,Tkach,Mamchur,Kovalenko, E. Yu.
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experimental part
p. 96 - 105
(2010/09/04)
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- N-substituted alpha-arylazacycloalkylmethanamines and their use as cardiovascular agents
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Novel compounds of the formula below wherein W is azetidine, pyrrolidine or piperidine, Q is a straight chain hydrocarbon radical of 1-4 carbons and may contain a double bond, and STR1 Ar is phenyl, pyridinyl or pyrimidinyl, a process for their preparation, and novel intermediates are disclosed. The novel compounds and the pharmaceutical compositions of this invention are useful in the treatment of hypertension, arrhythmias and angina.
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- Reactions of o-Aminonitriles with Isocyanates. 1. A Two-Step Synthesis of 2,6-Dihydroimidazoquinazolin-5-(3H)one
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The reaction of anthranilonitrile with 2-chloroethyl isocyanate yields 2-benzonitrile (6) which, upon heating, or treatment with base, undergoes a double cyclization to form 2,6-dihydroimidazoquinazolin-5-(3H)one (8) in excellent yield.When heated with hydrochloric acid, 6 is converted initially into 2-(2-chloroethylamino)-4H-benzoxazin-4-one (18) and further into 3-(2-chloroethyl)-2,4-(1H,3H)quinazolinedione (15).The acid-catalyzed reaction of 2,3-dihydro-5H-oxazoloquinazolin-5-one (14) with nucleophilic reagents yields 3-substituted 2,4-(1H,3H)quinazolinediones.
- Papadopoulos, Eleftherios Paul
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p. 1553 - 1558
(2007/10/02)
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