Ajinomoto Co., Ltd.

Toshihiro Matsuzawa

Takashi Tsuji

Tomoyuki Onishi

Noriyasu Kataoka

Masanobu Yatagai

Akinori Tatara

Shinichiro Takahashi

Seiichi Nishi

Tohru Nishiwaki

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

A process for purifying 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl) cycdopropane-1&prime;-yl&rsqb;methylpurine represented by the following formula (5) comprises the step of selectively isolating 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl) cyclopropane-1&prime;-yl&rsqb;methylpurine from a mixture of 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl)cyclopropane-1&prime;-yl&rsqb;methylpurine and 2-amino-6-chloro-7-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl)cyclopropane-1&prime;-yl&rsqb;methylpurine represented by the following formula (6) by the crystallization. This process has a satisfactory medicinal quality on an industrial scale without necessitating complicated operations such as chromatographic purification.

Process for isolating 2-amino-6-chloro-9-&lsqb;(1'S,2'R)-1'2'-bis(hydroxymethyl)-cyclopropane-1'-YL&rsqb;methylpurine and an optical isomer thereof

A pure (-)-9-[1'S, 2'R-bis(hydroxymethyl)cyclopropan-1'-yl]methylguanine is prepared by:

Method for purifying nucleic acid derivatives

A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo�3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Cyclopropane derivatives and method of preparing the same

An intermediate for the production of (3-oxo-2-oxobicyclo�3,1,0!hexan-1-yl) methanol represented by formula (II): ##STR1## selected from the group of compounds (9)-(11) as shown below, wherein R.sup.1 represents a lower alkyl group, R.sup.3 and R.sup.4 are each, independently, hydrogen or an alkyl group and M is an alkali metal or alkaline earth metal: ##STR2##

A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. In addition another aspect of the invention provides (3-oxa-2-oxobicyclo[3,1,0]hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

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Kawasaki, Japan

Toshihiro Matsuzawa