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79951644932
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Also known as ACT-178882.
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Also known as ACT-178882.
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33
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79951646415
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A% = HPLC area percent monitored at 220 nm.
-
A% = HPLC area percent monitored at 220 nm.
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34
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79951599177
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Other Pt-and Rh-based metals were also tested; however, much lower reactivities and/or purity profiles were observed.
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Other Pt-and Rh-based metals were also tested; however, much lower reactivities and/or purity profiles were observed.
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35
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3·THF see:;, and references therein
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39
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38049047508
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For a description of the microscale screening conditions utilized in this study see
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40
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0032558490
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Previous approaches to this class of intermediates include: (1) racemic hydrogenation followed by HPLC chiral separation
-
Previous approaches to this class of intermediates include: (1) racemic hydrogenation followed by HPLC chiral separation: Patane, M. A.; DiPardo, R. M.; Price, R. P.; Chang, R. S. L.; Ransom, R. W.; O'Malley, S. S.; Di Salvo, J.; Bock, M. G. Bioorg. Med. Chem. Lett. 1998, 8, 2495
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41
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84860702208
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Process for the preparation of enantiomerically enriched cyclic β-aryl or heteroaryl carboxylic acids. U.S. Pat. Appl. 2007/0232653 A1, (2) resolution of the racemic carboxylic acid: ref 16a; (3) asymmetric hydrogenation on the carboxylic acid: ref 16b.
-
Bachmann, S.; Scalone, M.; Schnider, P. Process for the preparation of enantiomerically enriched cyclic β-aryl or heteroaryl carboxylic acids. U.S. Pat. Appl. 2007/0232653 A1, 2007; (2) resolution of the racemic carboxylic acid: ref 16a; (3) asymmetric hydrogenation on the carboxylic acid: ref 16b.
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(2007)
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Bachmann, S.1
Scalone, M.2
Schnider, P.3
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42
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79951644044
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Other ligands tested: (S)-xyl-BINAP, (R, R)-Me-DuPhos, (R, R, S, S)-Tangphos, W006-1, Catasium I, J004-1 and J212-1 (structures are available in the Supporting Information)
-
Other ligands tested: (S)-xyl-BINAP, (R, R)-Me-DuPhos, (R, R, S, S)-Tangphos, W006-1, Catasium I, J004-1 and J212-1 (structures are available in the Supporting Information)
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43
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79951660067
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The Darco treatment is necessary to reduce the metal content in the product. Before treatment the levels are >20000 ppm.
-
The Darco treatment is necessary to reduce the metal content in the product. Before treatment the levels are >20000 ppm.
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44
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79951626143
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Isolation of the product and resubjecting the esters to the same epimerization conditions did not change the trans / cis ratio observed.
-
Isolation of the product and resubjecting the esters to the same epimerization conditions did not change the trans / cis ratio observed.
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45
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79951655996
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The rate of dissolution or solubility of different NaOEt sources in ethanol may explain the different results observed.
-
The rate of dissolution or solubility of different NaOEt sources in ethanol may explain the different results observed.
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46
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79951624817
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A full mechanism analysis is underway and will be reported in due course.
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A full mechanism analysis is underway and will be reported in due course.
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47
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79951606662
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Alternatively 10 equiv of TFA can be used with carefull monitoring of the KF.
-
Alternatively 10 equiv of TFA can be used with carefull monitoring of the KF.
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48
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79951616306
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Process for the preparation of diazabicyclo[3.3.1]nonane derivatives. WO 2008/088690 A2.
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Gauvreau, D.; Huffman, M. A.; Hughes, G.; Itoh, T.; Yin, J.; Lau, S.; O'Shea, P. Process for the preparation of diazabicyclo[3.3.1]nonane derivatives. WO 2008/088690 A2, 2008.
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(2008)
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Gauvreau, D.1
Huffman, M.A.2
Hughes, G.3
Itoh, T.4
Yin, J.5
Lau, S.6
O'Shea, P.7
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