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Pantoprazole Intermediate - PFBS Crystal Forms

IP.com Disclosure Number: IPCOM000016610D
Publication Date: 2003-Jul-03
Document File: 4 page(s) / 162K

Publishing Venue

The IP.com Prior Art Database

Abstract

5-Difluoromethyoxy-2-[[3,4-dimethyoxy-2-pyridinyl]methylthio]-1H benzimidazole (PFBS) is used as intermediate in the preparation of Pantoprazole. Various samples of PFBS were analyzed by X-Ray Powder diffraction and found to contain different cyrstal forms (A, B, C).

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16 June 2003

Pantoprazole intermediate - PFBS Crystal forms

5-difluoromethoxy-2-[[3,4-dimethoxy-2-pyridinyl]methylthio]-1H benzimidazole (PFBS) is used as intermediate in the preparation of Pantoprazole. Various samples of PFBS were analyzed by X-Ray Powder diffraction and found to contain different crystal forms (A,B,C). Table I summarizes the various samples and suppliers. XRD diffractograms of PFBS form A, B and C are shown in fig. 1-3. Main XRD peaks for the various forms A-C are listed in Table II. X-Ray Powder Diffractions were performed on ARL (Scintag) X-Ray powder diffractometer

model X'TRA, Cu-tube, solid state detector. A round standard aluminum sample holder with round zero background quartz plate was used. Scanning parameters: range 2-40 deg.2J, continuous scan, rate 3 deg/min.

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Table I

Sample Crystal form

Supplier: ZMC
Batch 20011201 Manufacturer: H Yannian MLT (HYM), China

Supplier: XIAMEN Batch:20011201 Manufacturer: H. Yatai Pharma (HYP)

Supplier: ZMC Batch 20030201 Manufacturer: H Yannian MLT (HYM), China

Supplier: SINOCHEM Batch:20030308 Manufacturer N. Yutai Chem

Supplier: XIAMEN Batch: 20030208 Manufacturer: H. Yatai Pharma (HYP)

A

Supplier: AUROBINDO, India BBatch PS -08001072 Supplier: TRUSTCHEM, China A Supplier: SINOCHEM
Batch: 20020401 Manufacturer N. Yutai Chem

C

A

A

A+B

A

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Table II

Crystal form XRD peaks

A 6.0, 12.0, 14.0, 14.4, 15.6, 16.5, 17.0, 17.7, 18.1,

18.7, 19.7, 21.7, 23.0, 24.3, 24.8, 25.4, 26.8

B 5.7, 7.0,...