cas 1256388-51-8, Ledipasvir | Articles data

Articles about 1256388-51-8Total 12 be found

Ledipasvir preparation method
The invention discloses a Ledipasvir preparation method. The Ledipasvir preparation method includes steps: (1) Ledipasvir intermediate product 1-LD-B preparation; (2) Ledipasvir intermediate product 2-LD-E preparation; (3) Ledipasvir intermediate product 3-LD-F preparation; (4) Ledipasvir intermediate product 4-LD-J preparation; (5) Ledipasvir intermediate product 5-LD-L preparation; (6) Ledipasvir-LD-Q preparation. The Ledipasvir preparation method has advantages of technical maturity and stability, product quality stability, safety and reliability in production process and suitableness for industrial production.
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(2018/05/16)

METHOD OF PREPARATION FOR LEDIPASVIR AND DERIVATIVE THEREOF, AND INTERMEDIATE COMPOUND FOR PREPARATION OF LEDIPASVIR
Methods of preparing Ledipasvir and derivatives thereof, and intermediate compounds used in the preparation of Ledipasvir are provided. Specifically, a method for preparing the compounds of formula 1 and a series of preparation methods of preparing Ledipasvir are provided. The methods described herein are simple and efficient, and have better application prospects.
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Paragraph 0203; 0204

(2018/04/14)

PROCESS FOR PREPARATION OF LEDIPASVIR
The present invention relates to a process for the preparation of ledipasvir a compound of formula I, which is useful as an antiviral agent. The present invention also provides ledipasvir phosphate.
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(2017/09/15)

Preparation method of ledipasvir
The invention belongs to the drug synthesis field and particularly relates to a preparation method of ledipasvir. The preparation method comprises the following steps: reacting by virtue of a compound (II) and a compound (III) under the action of alkali, so as to obtain a compound (IV); reacting by virtue of the compound (IV) and a compound (V) under the action of a metal catalyst, so as to obtain a compound (VI); reacting by virtue of the compound (VI) and an amine reagent, so as to obtain a compound (VII); reacting by virtue of the compound (VII) under the action of acid, so as to obtain a compound (VIII); and reacting by virtue of the compound (VIII) and Moc-L-valine under the action of a condensing agent, so as to obtain the ledipasvir represented by a chemical formula (I). The preparation method has the beneficial effects that the process route is short, the operation is simple and convenient, and the reaction yield is high.
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(2017/07/19)

AN IMPROVED PROCESS FOR THE PREPARATION OF LEDIPASVIR
The present invention provides an improved process for the preparation of compound of formula (I) and its pharmaceutical acceptable salts or solvates thereof, which is useful as an antiviral agent. This disclosure is also provides a process for the preparation of Ledipasvir key intermediates.
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Paragraph 17; 18

(2017/06/19)

Preparation method of ledipasvir and intermediate for preparing ledipasvir
The invention provides a preparation method of a ledipasvir key intermediate. The preparation method comprises the following steps: taking a compound with the structure shown as the formula I and 2-bromo-7-chloro-9-fluorene are used as starting materials and preparing a compound with the structure shown as the formula II and 2-bromo-7-chloro-9,9-difluoro-9H-fluorene respectively; carrying out a carbon-hydrogen activation coupling reaction, a Suzuki coupling reaction and a deprotection reaction to obtain the key intermediate for synthesizing ledipasvir, namely, a compound with the structure shown as the formula VIII; carrying out a condensation reaction on the key intermediate and Moc-L-valine, so as to obtain the ledipasvir. The preparation method of the ledipasvir key intermediate, provided by the invention, is simple and has a few of steps; the key compound, namely the 2-bromo-7-chloro-9,9-difluoro-9H-fluorene (formula IV), can be prepared into the key intermediate VIII for synthesizing ledipasvir through a three-step reaction; the utilization rate of a fluorine compound is improved and the preparation cost is reduced.
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(2017/07/26)

Preparation method of Ledipasvir
The invention discloses a preparation method of Ledipasvir. The method has no need for chromatographic column separation, reduces the cost of raw materials, and can acquire a high purity product by a simple precipitation or crystallization purification means, thus providing feasible technical conditions for large-scale industrial production.
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(2016/10/31)

PROCESS FOR THE PREPARATION OF LEDIPASVIR
Chemical synthetic methods useful for the synthesis of ledipasvir and pharmaceutically acceptable salts thereof are disclosed.
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(2017/04/11)

Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection
A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification of 39 (ledipasvir, GS-5885). Compound 39 (GT1a replicon EC50 = 31 pM) has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid >3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. 39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.
Link, John O.,Taylor, James G.,Xu, Lianhong,Mitchell, Michael,Guo, Hongyan,Liu, Hongtao,Kato, Darryl,Kirschberg, Thorsten,Sun, Jianyu,Squires, Neil,Parrish, Jay,Keller, Terry,Yang, Zheng-Yu,Yang, Chris,Matles, Mike,Wang, Yujin,Wang, Kelly,Cheng, Guofeng,Tian, Yang,Mogalian, Erik,Mondou, Elsa,Cornpropst, Melanie,Perry, Jason,Desai, Manoj C.
p. 2033 - 2046
(2014/04/03)

METHODS FOR TREATING HCV
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
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(2013/10/22)

SOLID FORMS OF AN ANTIVIRAL COMPOUND
Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.
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Paragraph 0265-0266

(2014/01/07)

METHODS FOR TREATING HCV
This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
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(2013/03/28)