Stella Pharma Corporation

Osaka Prefecture University Public Corporation

Yoshihide Hattori

Mitsunori Kirihata

Kohki Uehara

Hiroshi Takenaka

Tomoyuki Asano

Shintaro Kusaka

To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B&#x2014;H; &#x2014;Rrepresents &#x2014;(CH)n-X&#x2014;R(n represents an integer of 0 to 6; Xrepresents O, S, NH, S&#x2014;S, O&#x2014;CO, NHCO or SCO, or does not exist; Rrepresents C-Calkyl, hydroxy C-Calkyl, amino C-Calkyl, azido C-Calkyl, hydroxycarbonyl C-Calkyl, or the like), or a group having a repeating sequence of &#x2014;(CH)&#x2014;O&#x2014; 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and &#x2014;Ris &#x2014;(CH)m-X&#x2014;R(m represents an integer from 0 to 8; Xrepresents O, S, NH, S&#x2014;S, O&#x2014;CO, NHCO or SCO, or does not exist; and Rrepresents a tumor recognition moiety), or does not exist are prepared and used. 

Boron-containing compound

The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2]. 

Boron compound with amino acid skeleton containing cyclo ring-type ring

Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed. 

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Osaka, Japan

Yoshihide Hattori