- Preparation method of anagrelide impurities B
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The invention discloses a preparation method of anagrelide impurities B. The structure of the anagrelide impurities B is shown in formula I as shown in specification, and is obtained by nitratlon reaction, reduction reaction, halogenating reaction, conden
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Paragraph 0053; 0054
(2018/05/01)
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- PROCESS FOR THE PREPARATION OF ANAGRELIDE AND ANALOGUES THEREOF
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The present invention relates to a novel process for producing anagrelide, 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, or certain analogues thereof. The process of the invention also provides improved processes for producing key intermedia
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Paragraph 0091; 0092; 0093
(2013/08/28)
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- PROCESS FOR THE PREPARATION OF ANAGRELIDE AND ANALOGUES THEREOF
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The present invention relates to a novel process for producing anagrelide, 6,7-dichloro-1,5- dihydroimidazo [2,1-b] quinazolin 2 (3H)-one, or certain analogues thereof. The process of the invention also provides improved processes for producing key interm
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Page/Page column 23; 30
(2012/05/05)
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- PROCESS FOR THE PREPARATION OF ANAGRELIDE AND ANALOGUES
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The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases.
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Page/Page column 20-21
(2010/08/05)
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- Aminophenyl derivatives as selective androgen receptor modulators
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Disclosed herein is a novel class of aminophenyl compounds having the structure: wherein R1 is cyano or nitro and ring A is a bi- or tricyclic bridged heterocycle and to their use as modulators of androgen receptor for the treatment or preventi
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Page/Page column 21
(2008/06/13)
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- 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
(2010/02/13)
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- Method for the manufacture of anagrelide
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Methods are provided for making Anagrelide base from 2,3-dichlorobenzaldehyde. A method is also provided for making an intermediate compound ethyl N-(2,3-dichloro-6-nitrobenzyl)glycine from 2,3-dichlorobenzaldehyde and for reducing the glycine compound using either SnCl2 or a specially defined catalyst. A cyclization method to form Anagrelide base from the corresponding iminoquinazoline compound is further provided.
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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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