- HETEROCYCLYL SUBSTITUTED PYRROLOPYRIDINES THAT ARE INHIBITORS OF THE CDK12 KINASE
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This invention relates to compounds that are inhibitors of the CDK12 kinase. The compounds are useful in the treatment of disorders mediated by CDK12 kinase including myotonic dystrophy type 1 (DM1) and other disorders caused by the generation of RNA repeat expansion transcripts. In particular,the invention relates to compounds of the formula (I), or a pharmaceutically acceptable salts or N-oxides thereof, wherein R1a, R2, R3, R4a, R4b and R4c are as defined herein.
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Page/Page column 106; 107
(2019/04/16)
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- Synthesis of n.c.a. cis- and trans-4-[18F]fluoro-L-proline, radiotracers for PET-investigation of disordered matrix protein synthesis
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A radiosynthesis of n.c.a. (2S,4R)-4-[18F]fluoroproline (trans-configuration) and its diastereomer (2S,4S)-4-[18F]fluoroproline (cis-configuration) has been developed. It allows the routine production of up to 18 GBq of product for c
- Hamacher, Kurt
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p. 1135 - 1144
(2007/10/03)
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- Practical synthesis of Boc and Fmoc protected 4-fluoro and 4-difluoroprolines from trans-4-hydroxyproline
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Boc-cis-4-fluoro-L-proline and 4-difluoro-L-proline, usable in classical peptide synthesis, were obtained in respectively 71% (3 steps) and 65% (4 steps) overall yields from the readily available trans-4-hydroxy-L-proline methyl ester. The corresponding fluorinated trans-isomer was isolated in 24% yield (5 steps). Transformation of Boc-protected compounds to their Fmoc-equivalents was performed in high yields.
- Demange, Luc,Menez, Andre,Dugave, Christophe
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p. 1169 - 1172
(2007/10/03)
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- Synthesis of (2S)-4,4-difluoroproline, (2S,4R)-4-fluoroproline and their derivatives from (S)-aspartic acid
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Syntheses for (2S)-4,4-difluoroproline, (2S,4R)-4-fluoroproline and their derivatives are described starting from (S)-aspartic acid, using hexafluoroacetone as the protecting reagent and DAST as the fluorinating agent.
- Burger, Klaus,Rudolph, Martin,Fehn, Susanna,Sewald, Norbert
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