Daiichi Sankyo Company, Limited

Sankyo Company, Limited

Cyclacel Limited

Takashi Takita

Masashi Watanabe

Hiroshi Nagasawa

Noritada Sato

Michiaki Kawahara

Gen Hasegawa

Takahiro Okachi

Eiji Numagami

Robert Westwood

Gavin Wood

Tsuyoshi Murofushi

Keiichi Ohtsuka

Susumu Harashima

Gavin Jeffrey Wood

The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein Rrepresents a methyl group or a trifluoromethyl group, Rrepresents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide. 

Crystal of pyrrole derivative and method for producing the same

The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2' into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2&#x2032;-cyano-2&#x2032;-deoxy-N-palmitoyl-1-&#x3b2;-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer. 

Preparation of intermediates useful in the synthesis of 2'-cyano-2&#x2032;-deoxy-N4-palmi-toyl-1-&#x3b2;-D-arabinofuranosylcytosine

The present invention provides crystalline forms and compositions thereof, of a pyrimidine nucleoside derivative of formula (I) having anti-tumour activity, wherein formula (I) is:

Crystalline forms of pyrimidine nucleoside derivative

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Kanagawa, Japan

Takashi Takita