Yamasa Corporation

Kohei Yamada

Hiroyuki Hayakawa

Haruhiko Machida

Kazuki Endo

Yuichi Yoshimura

Mikari Watanabe

Satoru Kogo

Kazuomi Osawa

Kazuki Deguchi

Yuko Iwai

Noritake Matsumoto

A method for producing P,P-di(uridine 5'-)tetraphosphate (UPU) that can avoid reduction of the synthetic efficiency without using UTP free is developed. A method for producing UPU comprising reacting a phosphoric acid-activating compound represented by formula [II] or [III] with a phosphoric acid compound selected from the group consisting of UMP, UDP, UTP and a pyrophosphoric acid or a salt thereof (excluding UTP free) in water or a hydrophilic organic solvent, in the presence of a metal ion selected from the group consisting of an iron (II) ion, an iron (III) ion, a trivalent aluminum ion, a trivalent lanthanum ion, and a trivalent cerium ion. where, in the formula [II], Rrepresents a uridyl group binding to the 5&#x2032;-position, X represents a heterocyclic group, and n represents an integer of 1 or 2, where, in the formula [III], X represents a heterocyclic group selected from the group consisting of an imidazolyl group, a benzimidazolyl group, and a 1,2,4-triazolyl group. 

Method for producing P,P-di(uridine 5'-) tetraphosphate

A method for producing P,P-di(uridine 5'-)tetraphosphate (UPU) that can avoid reduction of the synthetic efficiency without using UTP free is developed. A method for producing UPU comprising reacting a phosphoric acid-activating compound represented by formula [II] or [III] with a phosphoric acid compound selected from the group consisting of UMP, UDP, UTP and a pyrophosphoric acid or a salt thereof (excluding UTP free) in water or a hydrophilic organic solvent, in the presence of a metal ion selected from the group consisting of an iron (II) ion, an iron (III) ion, a trivalent aluminum ion, a trivalent lanthanum ion, and a trivalent cerium ion. 

Method for producing P1,P4-di(uridine 5'-) tetraphosphate

In the present invention, a novel 2-alkynyl-N9-propargyladenine represented by formula (I) wherein Rrepresents a halogen atom, a furyl group, or a triazolyl group; Rand Reach represents a hydrogen atom or a C1-8 alkyl group, or form a cycloalkyl group by bonding to each other; and X represents a hydrogen atom or a hydroxyl group, or a pharmaceutically acceptable salt thereof, has a stronger and longer-lasting effect as a therapeutic agent for Parkinsonian syndromes.

2-alkynyl-N9-propargyladenine and medicinal use thereof

A di(pyrimidine nucleoside 5'-)polyphosphate is synthesized by converting a pyrimidine nucleoside 5&#x2032;-triphosphate into a pyrimidine nucleoside 5&#x2032;-cyclic triphosphate by use of a condensing agent, and subsequently reacting the pyrimidine nucleoside 5&#x2032;-cyclic triphosphate with a pyrimidine nucleotide in the presence of a salt of a metal selected from among magnesium, manganese, and iron. Through the method of the invention, a di(pyrimidine nucleoside 5&#x2032;-)polyphosphate can be synthesized from an unprotected pyrimidine nucleoside 5&#x2032;-phosphate serving as a starting material at a synthesis yield of 50% or higher. Therefore, the method of the invention is suitable for large-scale synthesis of a di(pyrimidine nucleoside 5&#x2032;-)polyphosphate.

Process for producing di(pyrimidine nucleoside 5'-)polyphosphate

A method for producing 2'-deoxy-2&#x2032;-fluoro-&#x3b2;-D-arabinonucleoside represented by formula (II): (wherein B represents a base), in particular, 2&#x2032;-deoxy-2&#x2032;-fluoro-&#x3b2;-D-arabinopurinenucleoside, which method comprises causing a nucleoside phosphorylase to act on &#x3b1;-1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (I): or a mixture of &#x3b1;- and &#x3b2;-isomers of 1-phosphorylated-2-deoxy-2-fluoroarabinoside represented by formula (V&#x2032;): and on a base. The compound can be produced at high yield and in a convenient and highly stereoselective manner.

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Choshi, Japan

Kohei Yamada