摘要:
The invention is directed to a process for the preparation of a cyclic carbamate starting with o- aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C 2-5 -alkyl C 2-5 -carboxylates and mixtures of at least one C 2-5 -alkyl C 2-5 -carboxylate with at least one C 5-8 -alkane.
摘要:
The present invention relates to compounds defined by formula I wherein the variables R 1x , R 2x , R 3x , R 4x , R 5x , R 6x , R 7x , R Nx , R 10x , A x , Z x and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta- HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要:
The invention is directed to a process for the preparation of a cyclic carbamate starting with o- aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C 2-5 -alkyl C 2-5 -carboxylates and mixtures of at least one C 2-5 -alkyl C 2-5 -carboxylate with at least one C 5-8 -alkane.
摘要:
The invention concerns the use of compounds of formula (I), wherein the radicals R1, R2 and R3 are such as defined in the description and the claims, for producing a drug for treating respiratory diseases as well as novel compounds of formula (I). The invention also concerns a method for producing said compounds, and pharmaceutical formulations containing them.
摘要:
The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.