Ajinomoto Co., Ltd.

Elobix Ab

Akinori Tatara

Noriyasu Kataoka

Ganapati Bhat

Michael Lofthagen

Johnson M Coutinho

Tamotsu Suzuki

Tatsuya Okuzumi

Masayuki Sugiki

Masanobu Yatagai

Tatsuhiro Yamada

Mikael Dahlström

Koichi Fujita

Toshihiro Matsuzawa

Shinichiro Takahashi

Kotaro Okado

Riho Kodama

Junko Yamanaka

Mikael Dahlstrom

Shinya Kiguchi

The present invention relates to a process for the preparation of a compound of formula (I) comprising: reacting a compound of formula (II) with a compound of formula (III) in the presence of a triazine compound to obtain a compound of formula (IV), and deprotecting said compound of formula (IV) to obtain the compound of formula (I). The compound of formula (I) can be prepared by the process according to the present invention in high yields and high purity. In addition, the process according to the present invention does not use a large amount of solvents or require a purification process of intermediate compounds.

Method for producing a 1,5-benzothiazepin compound

The present invention relates to a process for the preparation of certain 1,5-benzothiazepine compounds, and in particular to a process for the preparation of elobixibat. The process can be carried out under mild and safe conditions and may be used to prepare elobixibat on an industrial scale. The invention also relates to a process for the preparation of a crystalline monohydrate of elobixibat.

Process for the preparation of 1,5-benzothiazepine compounds

Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I). 

Crystals of salts of phenylalanine derivatives

A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c):  with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative;

Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives

The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having &#x3b1; 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like. 

Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof

The present invention releates to a method for preparing a phenylalanine compound having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof: 

Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of derivatives

The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly &#x3b1;-type, &#x3b3;-type, &#x3b5;-type, &#x3b7;-type, and &#x3b8;-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.

Crystals of phenylalanine derivatives and production methods thereof

The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of 

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Kawasaki, Japan

Akinori Tatara