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Amorphous form of magnesium bis[(S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3- methylureido)-4-morpholinobutanoate]

IP.com Disclosure Number: IPCOM000236227D
Publication Date: 2014-Apr-13
Document File: 2 page(s) / 15K

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Amorphous form of magnesium bis[(S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3- methylureido)-4-morpholinobutanoate]

1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3- thiazol-4-yl]methyl}carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6- diphenylhexan-2-yl]carbamate, referred to as Compound I.

    Described herein is a process for preparing magnesium bis[(S)-2-(3-((2- isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoate], referred to as compound II, which is an intermediate in the preparation of compound I. Samples of Compound II were prepared by the process described in example 1, and were analyzed by X-ray powder diffraction ("XRPD") to provide an amorphous form. Figure 1 presents the XRPD of the obtained product.

Figure 1: XRPD of the amorphous form of Compound II

2000

XRPD method

    The analysis was performed on ARL (SCINTAG) powder X-Ray diffractometer model X'TRA equipped with a solid state detector. Copper radiation of
1.5418 Å was used. Scanning parameters: range: 2-40 degrees two-theta; scan mode: continuous scan; step size: 0.05°, and a rate of 3 deg/min.

Example 1: Process for preparing (magnesium bis[(S)-2-(3-((2-isopropylthiazol-4-

yl)methyl)-3-methylureido)-4-morpholinobutanoate] (Compound II)

    A 100 mL reactor was charged with methyl (S)-2-(3-((2-isopropylthiazol-4- yl)methyl)-3-methylureido)-4-morpholinobutanoate oxalate (15 g), Mg(OH)2 (2.95 g)

1600

1200

CPS

800

400

0


2.0


6.0


10.0


14.0


18.0


22.0


26.0


30.0


34.0

...