Concepedia

Kilogram-Scale Synthesis of a Highly Selective α<sub>1</sub>-Adrenoceptor Antagonist (DL-028A)

Shan‐Yen Chou, Wei‐Kung Yin, Yuh-Shan Chung, Lien‐Shange Chang, Chin‐Wei Liu, Shyh‐Fong Chen, Kae‐Shyang Shih

Organic Process Research & Development · 2002 · 15 citations · 5 references

DOI

Concepts

Abstract

This work presents an improved eight-step process, leading to kilogram quantities of high-quality DL-028A, an antihypertensive agent. The improvements include reducing the levels of toxic reagents and the removal of dangerous processes and waste gas treatment. Moreover, specification and impurity profiles were determined.

References

5

Studies on quinazolines. 5. 2,3-Dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective .alpha.1-adrenoceptor antagonists and antihypertensive agents

Ji Wang Chern, Pao Luh Tao, M.‐H. YEN et al. · Journal of Medicinal Chemistry · 1993 · 74 citations · Full text

, , +9

Evidence that blood pressure reduction by serotonin antagonists is related to alpha receptor blockade in spontaneously hypertensive rats.

Marlene L. Cohen, Ray W. Fuller, K D Kurz · Hypertension · 1983 · 66 citations · Full text

, , +17

Further evaluation of the selectivity of a novel antihypertensive agent, SGB-1534, for peripheral α1-adrenoceptors in the spinally anestherized dog

Jun‐ichi Imagawa, Kazushige Sakai · European Journal of Pharmacology · 1986 · 38 citations

, , +10

Electrical and mechanical properties of the capsular smooth muscles of the rabbit prostate in relation to the actions of the α<sub>1</sub>‐adrenoceptor blocker, YM‐12617

Narihito Seki, Eiichiro Nishiye, Takeo Itoh et al. · British Journal of Pharmacology · 1988 · 17 citations · Full text

, , +15

Studies on quinazolines. 6. Asymmetric synthesis of (S)-(+)- and (R)-(−)-3-[[4-(2-methoxyphenyl)piperazin-1-yl]methyl]-5-methylthio-2,3-dihydroimidazo[1,2-c]quinazolines

A. GUTCAIT, Kuang-Chao Wang, Liu Hsiu-Wen et al. · Tetrahedron Asymmetry · 1996 · 12 citations

, , +12