1422894-88-9Relevant academic research and scientific papers
Facile entry to an efficient and practical enantioselective synthesis of a polycyclic cholesteryl ester transfer protein inhibitor
Han, Zhengxu S.,Xu, Yibo,Fandrick, Daniel R.,Rodriguez, Sonia,Li, Zhibin,Qu, Bo,Gonnella, Nina C.,Sanyal, Sanjit,Reeves, Jonathan T.,Ma, Shengli,Grinberg, Nelu,Haddad, Nizar,Krishnamurthy, Dhileep,Song, Jinhua J.,Yee, Nathan K.,Pfrengle, Waldemar,Ostermeier, Markus,Schnaubelt, Juergen,Leuter, Zeno,Steigmiller, Sonja,Daeubler, Juergen,Stehle, Emanuel,Neumann, Lukas,Trieselmann, Thomas,Tielmann, Patrick,Buba, Annette,Hamm, Rainer,Koch, Gunter,Renner, Svenja,Dehli, Juan R.,Schmelcher, Florian,Stange, Christian,MacK, Juergen,Soyka, Rainer,Senanayake, Chris H.
supporting information, p. 4142 - 4145 (2014/10/15)
An efficient enantioselective synthesis of the chiral polycyclic cholesteryl ester transfer protein (CETP) inhibitor 1 has been developed. The synthesis was rendered practical for large scale via the development of a modified Hantzsch-type reaction to prepare the sterically hindered pyridine ring, enantioselective hydrogenation of hindered ketone 6 utilizing novel BIBOP-amino-pyridine derived Ru complex, efficient ICl promoted lactone formation, and a BF3 mediated hydrogenation process for diastereoselective lactol reduction. This efficient route was successfully scaled to produce multikilogram quantities of challenging CETP drug candidate 1.
Crystalline forms of a hexahydrofuro[3,4-c]quinoline derivative
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, (2013/08/28)
The present invention relates to crystalline forms of (3R,9S)-4-isopropyl-7,7-dimethyl-3-(4-(trifluoromethyl)phenyl)-2′,3′,5′,6,6′,7,8,9-octahydro-3H-spiro[furo[3,4-c]quinoline-1,4′-pyran]-9-ol and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.
CRYSTALLINE FORMS OF OCTAHYDRO-3H-SPIRO [FURO [3, 4-C] QUINOLINE -1, 4 '-PYRAN] -9-OL
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, (2013/03/26)
The present invention relates to crystalline forms of the compound of formula (I) as shown in the description and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.
