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(S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl acetamide intermediates

IP.com Disclosure Number: IPCOM000029292D
Publication Date: 2004-Jun-22
Document File: 3 page(s) / 146K

Publishing Venue

The IP.com Prior Art Database

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Page 1 of 3

(S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazoli acetamide intermediates


I) (R)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl azide, purchased from Dankong Industry & trade group Co., LTD, is used as an intermediate in the preparation of (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo- 5-oxazolidinyl]methyl acetamide.

Its structure is as follows:

O

N

F N

O

O

(R)

CH2N3

           C14H16FN5O3 Mol. Wt.: 321.31 C, 52.33; H, 5.02; F, 5.91; N, 21.80; O, 14.94

FMO-N3

Pattern #1: Main XRD peaks for the pattern 1 are: 6.0; 14.7; 22.4; 23.0; 23.7; 24.3; 24.3; 25.2;


26.4; 27.8; 29.7.

22500

CPS

FMO-N3 crystal form I

21500

20500

19500

18500

17500

16500

15500

14500

13500

12500

11500

10500

9500

8500

7500

6500

5500

4500

3500

2500

1500

500 5.0

8.0

38.0

Deg.

2.0

11.0

14.0

17.0 20.0 23.0 26.0 29.0 32.0 35.0

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II) (R)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5- oxazolidinyl]methanol, purchased from Dankong Industry & trade group Co., LTD, is used as an intermediate in the preparation of (S)-N-[[3-[3-fluoro-4-(4- morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl acetamide. Its structure is as follows:

Pattern #2: Main XRD peaks for the pattern 2 are: 9.4; 15.3; 16.4; 17.2; 20.5; 21.0; 22.4; 23.6;
24.2; 31.0.

O

N

F N

O

O

CH2OH

          C14H17FN2O4 Mol. Wt.: 296.29 C, 56.75; H, 5.78; F, 6.41; N, 9.45; O, 21.60

(R)

FMO-OH

45000

CPS

FMO-OH crystal form II

43000

41000

39000

37000

35000

33000

31000

29000

27000

25000

23000

21000

19000

17000

15000

13000

11000

9000

7000

5000

3000

1000

5.0

11.0

38.0

Deg.

2.0

8.0

14.0

17.0 20.0 23.0 26.0 29.0 32.0...