Diastereoselective anodic hetero- and homo-coupling of menthol-, 8-methylmenthol- and 8-phenylmenthol-2-alkylmalonates
Diastereoselective radical coupling was achieved with chiral auxiliaries. The radicals were generated by anodic decarboxylation of five malonic acid derivatives. These were prepared from benzyl malonates and four menthol auxiliaries. Coelectrolyses with 3,3-dimethylbutanoic acid in methanol at platinum electrodes in an undivided cell afforded hetero-coupling products in 22-69% yield with a diastereoselectivity ranging from 5 to 65% de. Electrolyses without a coacid led to diastereomeric homo-coupling products in 21-50% yield with ratios of diastereomers being 1.17:2.00:0.81 to 7.03:2.00. The stereochemistry of the new stereogenic centers was confirmed by X-ray structure analysis and 13C NMR data.
Letzel, Matthias C.,Sch?fer, Hans J.,Fr?hlich, Roland
supporting information
p. 33 - 42
(2017/02/15)
PREVENTION AND TREATMENT OF OCULAR CONDITIONS
The present invention relates to pharmaceutical compositions comprising hydrogel-linked prodrug for use in the treatment, prevention and/or diagnosis a condition of the eye and ophthalmic devices comprising said pharmaceutical compositions.
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Paragraph 0934-0936
(2017/08/01)
VEGF NEUTRALIZING PRODRUGS FOR THE TREATMENT OF OCULAR CONDITIONS
The present invention relates to a pharmaceutical composition comprising one or more pharmaceutically acceptable excipient(s) and a VEGF neutralizing prodrug, which comprises a VEGF neutralizing biologically active moiety, for use in a method for the treatment of one or more ocular conditions.
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Page/Page column 118; 119
(2014/05/07)
DIAGNOSIS, PREVENTION AND TREATMENT OF DISEASES OF THE JOINT
The present invention relates to apolymeric prodrug for use in the treatment, prevention and/or diagnosis a disease of the joint and pharmaceutical compositions and medical devices comprising said polymeric prodrugs.
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Page/Page column 138; 139
(2014/05/07)
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