# US 2014/0194615 A1 · Method for the preparation of 2-[4-[(methylamino)carbonyl]-1-h-pyrazol-1-yl]adenosine monohydrate

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- Number: US 2014/0194615 A1
- Document ID: US20140194615A1
- Status: Published application
- Kind: A1
- Application number: 14/239,788
- Filed: 2012-08-14
- Published: 2014-07-10
- Earliest claimed: 2011-08-22
- Assignees: Farmak, A.S.
- Applicants: Farmak, A.S.
- Inventors: Lubomir Kvapil; Pavel Hradil; Martin Grepl; Petr Slezar; Barbora Dvorakova
- Web page: https://patentgrep.com/patent/US20140194615A1

## CPC

- C07H 19/16: Purine radicals
- C07H 19/167: with ribosyl as the saccharide radical
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)

## Abstract

A method for the preparation of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I by reaction of 2-(4-methoxycarbonylpyrazol-1-yl) adenosine of formula III with a solution of methylamine in a non-aqueous solvent, optionally in combination with another inert solvent, to produce anhydrous 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine, which is converted to 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yljadenosine monohydrate of formula I by addition of water.

## Claims

### Claim 1

A method for the preparation of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I
comprising the steps of:
a) reacting 2-(4-methoxycarbonylpyrazol-1-yl)adenosine of formula III
with methylamine in a non-aqueous solvent to produce anhydrous 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine,
b) adding water to the product of step a) to produce of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I.

### Claim 2

(canceled)

### Claim 3

(canceled)

### Claim 4

(canceled)

### Claim 5 (depends on 1)

The method according to claim 1, wherein the non-aqueous solvent is an alcohol or a polar aprotic solvent or a combination thereof.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the alcohol is methanol or ethanol.

### Claim 7 (depends on 5)

The method according to claim 5, wherein the polar aprotic solvent is dimethyl sulfoxide.