Substituted heterocyclo-norbornylamine derivatives, method for producing the same, their use as medicament or diagnostic agent and medicament containing the same .

Substituted heterocyclo-norbornylamine derivatives, method for producing the same, their use as medicament or diagnostic agent and medicament containing the same

Номер патента: EP1345902B1
Опубликовано: 01-06-2005
Автор(ы): Hans-Jochen Lang, Hans-Willi Jansen, Klaus Wirth, Uwe Heinelt
Принадлежит: Aventis Pharma Deutschland GmbH
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Рисунок 1. Взаимосвязь патентов (ближайшие 20).

Substituted heterocyclo-norbornylamine derivatives, method for producing the same, their use as medicament or diagnostic agent and medicament containing the same

Номер патента: CA2432208A1. Автор: Hans-Jochen Lang,Uwe Heinelt,Klaus Wirth,Hans-Willi Jansen. Владелец: Individual. Дата публикации: 2002-08-29.

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Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agent

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Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agents

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Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents

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METHOD FOR PREPARING 2-ARYL-1,2-DIHYDROCHINAZOLINES1 The invention relates to a new method for producing new substituted 1,2-dihydroquinolines, which can be used as intermediates for the synthesis of physiologically active compounds. A method for producing 1,2-dihydroquinazoline with hydrocarbon non-aromatic substituents in the dihydropyrimidine ring by reacting 5-chloro-2-aminobenzophenone oxime with acetone followed by treatment of the reaction product with phosphorus trichloride. This method, however, cannot be applied for the synthesis of 2-aryl-monosubstituted 1,2-dihydroquinazolines. According to the proposed method, 2-aryl-1,2-di-hydroquinazolines of the formula 1CH7HG, where R is hydrogen and methyl radical, Ar-phenyl or p-chlorophenyl radical, by the interaction of 1-aralk'Ilindazoles of the formula II, where R and Ar have the indicated meanings, with phenylmagnesium bromide in the medium B10 in the presence of 1,2-dimethoxyethy (DME) at the boiling point of the mixture. The resulting N-magnesium derivative of 2-aryl-1,2-dihydroquinazoline is subjected to hydrolysis, after which the free base is isolated.15 The structure of 2-aryl-1,2-dihydroquinazolines is proved by the conversion of 2-phenyl-1,2-dihydroquinazoline to the known compounds. Example 1. To phenylmagnesium bromide prepared from 1.04 g

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