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Table 1 Comparison of the efficiency of three different coupling methods for the synthesis of MRS7216 8a.

From: Novel alendronate-CGS21680 conjugate reduces bone resorption and induces new bone formation in post-menopausal osteoporosis and inflammatory osteolysis mouse models

Screening of coupling reagents and conditions

Sr. No.

Solvents, Reagents, and conditions

1 ā†’ 7a

7a ā†’ 8a

1.

DMF, EDC.HCl, NHS, DIPEA, rt,18h, 5a/ alendronic acid (in H2O), rt, 18h

58%

6%

2.

DMF, HATU, DIPEA, rt, 45min, 5a/ A [TBA]3, rt, 3h

70%

45%

3.

DMF, COMU, DIPEA, rt, 45min, 5a/ A [TBA]3, rt, 3h

78%

-

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Arthritis Research & Therapy

ISSN: 1478-6362

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