以IR及UV法监测阿法骨化醇合成反应进程
A Method for Monitoring the Process of Synthetic Reaction of Alfacalcidol by IR and UV

作者: 王 敏 * , 王明刚 :青岛正大海尔制药有限公司,青岛;

关键词: 阿法骨化醇IR及UV监测Alfacalcidol IR and UV Monitor

摘要:

目的:成阿法骨化醇,准确监测反应进程并判定反应终点。方法:IRUV法监测阿法骨化醇合成反应进程。结果:IRUV法能准确有效的监测阿法骨化醇合成反应进程,避免了反应不完全或过度反应导致副产物增加的弊端,提高了反应收率,且重现性好,收率稳定。结论:本方法操作简单、迅速、准确、有效,适合于工业化生产。
Objective: This paper is about synthetizing alfacalcidol, monitoring the reaction process and determining the end of the reaction. Method: Monitoring the process of the synthetic reaction of alfacalcidol by IR and UV. Results: This is an effective method to monitor the synthesis process and avoid the incomplete reaction or the overreaction, which can lead to the increase of the side product. Furthermore, the method increases the yield of the reaction and improves the good reproducibility. The yield is stable. Conclusion: The method is easy, rapid and accurate. It is suitable for the pharmaceutical manufacture.

文章引用: 王 敏 , 王明刚 (2013) 以IR及UV法监测阿法骨化醇合成反应进程。 药物化学, 1, 9-13. doi: 10.12677/HJMCe.2013.12003

参考文献

[1] Posner GH and Kahraman M. (2003) Organic chemistry of vita- min D analogues (deltanoids). European Journal of Organic Chemistry, 20, 3889- 3895.

[2] Babina M, Krautheim M, Grutzkau A, et al. (2000) Human leukemic mast cells (HMC-1) are responsive to 1-alpha, 25- dihydroxyvitamin D3: Selective promotion of ICAM- 3 ex- pression and constitutive presence of vitaminD3 receptor. Bio- chemical and Biophysical Research Communications, 273, 1104- 1110.

[3] Li XY, Boudjelal M, Xiao JH, et al. (1999) 1, 25-di- hydroxyvitamin D3 increase nuclear vitamin D receptors by blocking ubiquitin/proteasome-mediated degradation in human skin. Molecular Endocrinology, 13, 1686-1694.

[4] Chen TC, Schwartz GG, Burnstein KL, et al. (2000) The in vitro evaluation of 25-hydroxyvitamin D3 and 19-nor-1,25-dihydroxy- vitamin D2 as therapeutic agents for prostate cancer. Clinical Cancer Research, 6, 901-908.

[5] Brown AJ. (2001) Therapeutic uses of vitamin D analogues. American Journal of Kidney Diseases, 38, 3-19.

[6] Goltzman D, Miao DS, Panda DK, et al. (2004) Effect of cal- cium and the vitamin D system on skeletal and calcium homeo- stasis: lessons from genetic models. The Journal of Steroid Bio- chemistry and Molecular Biology, 89-90, 485-489.

[7] Yamada S, Shimizu M and Yamamoto K. (2003) Structure- function relationships of vitamin D including ligand recognition by the vitamin D receptor. Medicinal Research Reviews, 23, 89- 115.

[8] Enrico G. Baggiolini, Jerome A. Iacobelli and Bernard M. (1986) Hennessy, stereocontrolled total synthesis of 1, 25-dihydroxy- cholecalciferol and 1, 25-Dihydroxycholecalciferol. The Journal of Organic Chemistry, 51, 3098-3105.

[9] William S. Johnson, John D. Elliott and Gunnar J. (1984) Hanson asymmetrie synthesis via acetal templates.6.a stereo- selective approach to a key intermediate for the preparation of vitamin D metabolites. Journal of the American Chemical So- ciety, 106, 1138-1139.

[10] Paaren HE, Deluca HF and Schnoes HK. (1980) Direct C(1) hy- droxylation of vitamin D3 and related compounds. The Journal of Organic Chemistry, 45, 3253-3258.

[11] Tadashi Sato, Hiroshi yamauchi and Yoshitake Ogata. (1978) Studies on 1-hydroxyl derivatives of vitamin D3. I. syntheses of 1-hydroxyvitamin D3 and 1,25-dihydroxyvitamin D3. Chemical and Pharmaceutical Bulletin, 25, 2983-2940.

[12] DeLuca. (1985) Method for preparing 1-hydroxyvitamin D compounds. US 4554106.

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