- Method for synthesizing moxifloxacin and derivatives thereof
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The invention provides a method for synthesizing moxifloxacin and derivatives thereof. Aminopyrrolidone derivatives are constructed to further obtain (S,S)-2,8-diazo-bicyclo[4.3.0]nonane so as to synthesize the moxifloxacin and the derivatives thereof. The method has the beneficial effects that raw materials are wide in source and low in price; chiral resolution is not needed in a preparation process; the yield and purity are relatively high; the process cost is further reduced; obvious economic value is achieved.
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Paragraph 0024-0028
(2019/10/01)
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- New moxifloxacin impurity and preparation method and use thereof
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The invention provides a new moxifloxacin impurity and provides a preparation method and use as an impurity control of the new impurity. A commercially available bulk simple chemical is used as a starting material to construct a chiral dual ring, and further an impurity compound is synthesized; the reaction process has no need of chiral resolution; in addition, the operation is simple, the reaction condition is mild, and the application prospect is good. The moxifloxacin prepared by the invention has high impurity purity, and effectively ensures the purity of the impurity control and the accuracy of analysis work.
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Paragraph 0054-0058
(2019/10/01)
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- Synthetic method for moxifloxacin chiral side chain intermediate
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The invention provides a synthetic method for a moxifloxacin chiral side chain intermediate. The method provided by the invention uses an easily-available and inexpensive L-asparagine as a starting material to obtain the moxifloxacin chiral side chain intermediate through an eight-step reaction; and the whole route has novel design and avoids a chiral separation process adopted by most routes, andthe method has higher practicability, a high yield, a quick reaction speed and few by-products, and is very suitable for industrial application.
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Paragraph 0019-0023
(2019/10/01)
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- Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312
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Investigation of conformationally restricted benzamide bioisosteres led to the chiral phenyltetrahydropyrimidine derivative ent2a (FAUC 312) displaying strong and highly selective dopamine D4 receptor binding (Kihigh=1.5 nM). Mitogenesis experiments indicated 83% ligand efficacy when compared to the unselective agonist quinpirole. The target compounds of type 2 and 3 were synthesized in enantiopure form starting from asparagine.
- Einsiedel, Juergen,Huebner, Harald,Gmeiner, Peter
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p. 851 - 854
(2007/10/03)
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- Rotihibins, novel plant growth regulators from Streptomyces graminofaciens
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In the course of screening search for plant growth regulators, a culture filtrate of Streptomyces graminofaciens 3C02 was found to inhibit the growth of lettuce seedlings. The active substances, named rotihibin A (1) and B (2), were revealed to be lipo-peptidal compounds. Rotihibins inhibit growth of various plants at below 1 μg/ml, but do not show lethal activity even at higher doses.
- Fukuchi,Furihata,Nakayama,Goudo,Takayama,Isogai,Suzuki
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p. 1004 - 1010
(2007/10/03)
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