- METHOD FOR THE PRODUCTION OF ANAGRELIDE HYDROCHLORIDE
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Disclosed is a method for producing 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazoline-2(3H)-on hydrochloride (anagrelide hydrochloride). Said method comprises the following steps: a) 2,3-dichlorobenzaldehyde is nitrated to obtain 2,3-dichloro-6-nitrobenzaldehyde; b) 2,3-dichloro-6-nitrobenzaldehyde is reacted with hydroxylamine HCl and acetic anhydride by applying heat so as to obtain 2,3-dichloro-6-nitrobenzonitrile; c) the nitro group of 2,3-dichloro-6-nitrobenzonitrile is reduced to obtain 2,3-dichloro-6-aminobenzonitrile; d) the nitrile group of 2,3-dichloro-6-aminobenzonitrile is reduced to obtain 2,3-dichloro-6-aminobenzylamine dihydrochloride; e) 2,3-dichloro-6-aminobenzylamine dihydrochloride is reacted with i) bromoacetic acid ethyl ester, CH3CN, and triethylamine; and ii) BrCN to obtain (2-amino-5,6-dichloro-4H-quinazoline-3-yl) acetic acid ethyl ester; f) (2-amino-5,6-dichloro-4H-quinazoline-3-yl) acetic acid ethyl ester is reacted in cycloalkylation conditions to obtain 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazoline-2(3H)-on; and g) 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazoline-2(3H)-on is reacted with HCl to obtain anagrelide hydrochloride.
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Page/Page column 4-5
(2010/02/13)
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- 2-amino-5,6-dichloro-3,4-dihydroquinazoline, its method of making and using and pharmaceutical compositions thereof
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The compound 2-amino-5,6-dichloro-3,4-dihydroquinazoline has been found to have enhanced platelet count reducing properties. Also provided are methods for synthetically making the compound and a method of reducing the platelet count in a patient by administering to the patient a platelet reducing effective amount of the compound preferably together with a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which contains the above compound as the active ingredient together with pharmaceutically acceptable excipients.
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- Alkyl 5,6-dichloro-3,4-dihydro-2(1H)-iminoquinazoline-3-acetate hydrohalides
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The known blood platelet antiaggregative agent 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one is prepared in high yield via an improved process involving a novel intermediate of the Formula STR1 in which R1 is (lower)alkyl and X is bromo, chloro or iodo. Two processes for the preparation of compounds of the Formula III are disclosed, one of which involves the novel intermediate STR2
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