224161-38-0Relevant articles and documents
Chemo-Enzymatic One-Pot Two-Step Functionalization of 1,2,3,4-Tetrahydroisoquinolines by Monoamine Oxidase-Ugi-Joullié Reaction Sequence
Barna, Bence,Gáti, Tamás,Kotschy, András,Tasnádi, Gábor
supporting information, (2022/03/01)
A one-pot two-step chemo-enzymatic approach for the functionalization of substituted 1,2,3,4-tetrahydroisoquinolines (THIQs) was developed. The system combines monoamine oxidase (MAO)-catalyzed imine formation with Ugi-type three-component reaction in an aqueous buffer without intermediate isolation. The two steps were separately optimized for buffer and pH to obtain the expected products. MAOs enabled the functionalization of fifteen THIQs by oxidation to imines, while the Ugi-Joullié-reaction was successfully carried out with eight carboxylic acids and eight isonitriles. 41 products were isolated giving access to valuable building blocks for medicinal chemistry applications. Gram-scale transformation demonstrated the utility of the described protocol for organic synthesis.
COMPLEMENT PATHWAY MODULATORS AND USES THEREOF
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Page/Page column 104; 105, (2014/01/09)
The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Process for the preparation of (8As,12AS,13AS)-decahydroisoquino ((2,1-G) (1,6)-naphthyridin-8-one derivatives
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, (2008/06/13)
The invention provides a process for preparing single enantiomers of compounds represented by the formula: STR1 and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy; which includes reduction of a compound represented by the formula: STR2 to give a mixture of stereoisomers represented by the formula: STR3 wherein each wavy line independently represents a bond in either the α or β position; followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.