- A process for preparing A [...] sulfate method
-
A disclosed method for preparing A type atazanavir sulfate comprises the following steps: step a) adding atazanavir free alkali into an organic solvent to prepare a transparent solution at a controlled temperature of 10-65 DEG C, wherein the organic solve
- -
-
Paragraph 0029; 0032; 0035; 0038; 0041
(2018/04/20)
-
- TABLETED COMPOSITIONS CONTAINING ATAZANAVIR
-
Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.
- -
-
Paragraph 0098; 0099; 0100; 0101; 0102; 0103
(2018/06/01)
-
- A process for preparing a sulfuric acid Atazanavir method (by machine translation)
-
A is applied to the technical field of drug synthesis in the puma monomer as the raw material to prepare sulfuric acid Atazanavir method, the preparation method comprises the following steps: the puma monomer uses ethanol to dissolve after the dilution, t
- -
-
Paragraph 0018; 0019; 0020; 0021
(2017/08/29)
-
- A atazanavir bisulfate method for preparing A-type crystallization (by machine translation)
-
The invention discloses a atazanavir bisulfate method for preparing A-type crystallization, comprising the following steps: a) the application of the free base in ethanol, stir at room temperature, then dropping concentrated sulfuric acid, the reaction liquid heating and stirring, and then to add inert solvent, cooling crystallization, filtration and dried to obtain application E-type crystallization ethanol composition; wherein the molar concentration of the concentrated sulfuric acid is preferably 15-18.4mol/L; b) step 1) ethanol compound is obtained in the acetone E-type crystallization, heating to reflux stirring, cooling, filtering, and dried to obtain atazanavir bisulfate A-type crystallization. Preparation method of the invention aims of the invention, the operability of the process, improved product appearance property, improve the quality and purity of the product. (by machine translation)
- -
-
Paragraph 0026
(2016/12/12)
-
- PROCESS FOR THE PREPARATION OF ATAZANAVIR BISULFATE
-
The present invention relates to an improved process for the preparation of Atazanavir bisulfate Form A. The present invention also relates to a pharmaceutical composition using the Atazanavir bisulfate Form A of the invention.
- -
-
Paragraph 0086; 0087
(2015/07/15)
-
- PROCESS FOR PREPARING ATAZANAVIR SULPHATE
-
The present invention relates to a process for the preparation of Compound (A): (Formula (A)) wherein the process comprises contacting atazanavir base (Compound (II)) with sulphuric acid in a combination of two or more solvents and isolating compound (A).
- -
-
Page/Page column 20; 21
(2014/09/03)
-
- PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT
-
The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy-phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)—N—(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt.
- -
-
Paragraph 0086; 0087; 0088; 0089
(2014/12/09)
-
- Process for Preparing Form A of Atazanavir Sulfate
-
A process of making Form A of atazanavir sulfate comprises: a) mixing atazanavir free base with a solvent selected from the group consisting of methanol (MeOH), ethanol (EtOH), isopropanol (IPA), N-methylprrolidone (NMP) and combinations thereof; b) react
- -
-
Paragraph 0040
(2013/03/26)
-
- PROCESS FOR PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT
-
The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy- -phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)-N-(N-methoxycarbonyl-(L)-tert- leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt.
- -
-
Page/Page column 21-22
(2013/03/26)
-
- PROCESS FOR THE PREPARATION OF ATAZANAVIR SULFATE SUBSTANTIALLY FREE OF DIASTEREOMERS
-
The present invention provides atazanavir sulfate substantially free of diastereomeric impurities. The present invention also provides atazanavir sulfate having D-tertiary leucine analogues less than 0.1%. The present invention further relates to an improved process for preparing atazanavir sulfate, substantially free of its diastereoisomeric impurities, which comprises of reacting diamino compound (IV) with N-methoxycarbonyl-(L)-tertiary-leucine (V) having D-isomer less than 0.1 % to obtain atazanavir base; conversion of atazanavir base to atazanavir sulfate by reacting with sulfuric acid and crystallization of atazanavir sulfate from suitable organic solvent(s).
- -
-
Page/Page column 17
(2011/10/03)
-
- PREPARATION PROCESS OF AN ANTIVIRALLY HETEROCYCLIC AZAHEXANE DERIVATIVE
-
A process for the preparation of atazanavir or its pharmaceutically salts, or its solvates, which comprises condensing N-(methoxycarbonyl)-L-tert-leucine and 1-[4-(piridyn-2-yl)phenyl-4(S)-hydroxy]-5-(S)-2,5-diamino-6-phenyl-2-azahexane or a salt thereof using N,N-diisopropylcarbodiimide or N,N-dicyclohexylcarbodiimide and a tertiary organic amine, being the condensation carried out in the absence of 1-hydroxy-benzotriazole.
- -
-
Page/Page column 12
(2010/12/31)
-
- Process for preparing atazanavir bisulfate and novel forms
-
A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.
- -
-
Page/Page column 13
(2008/06/13)
-
- Process research and development for an efficient synthesis of the HIV protease inhibitor BMS-232632
-
Development of an efficient and scalable process for the human immunodeficiency virus (HIV) protease inhibitor BMS-232632 1-[4-(pyridin-2-yl)phenyl]-5(S)-2,5-bis{[N-(methoxycarbonyl)L-tert- leucinyl]-amino}-4(S)-hydroxy-6-phenyl-2-azahexane, is described. The key step in the synthesis of the intermediate N-1-(tert-butyloxycarbonyl)-N-2-[4-(pyridin-2-yl)benzylidene]hydrazone (11) was the Pd-mediated coupling of boronic acid 9 with 2-bromopyridine. An efficient procedure was developed for the chemoselective reduction of hydrazone 11 to hydrazine carbamate 4. The key intermediate N-(tert-butyloxycarbonyl)-2(S)-amino-1-phenyl-3(R)-3,4-epoxy-butane (6) was prepared stereoselectively from chiral diol 10. The subsequent union of 4 and 6 followed by coupling with N-methoxycarbonyl-L-tert-leucine provided the free base BMS-232632 in high yield. Evaluation of a variety of salts and identification of bisulfate salt 19 with enhanced bioavallability are also described.
- Xu, Zhongmin,Singh, Janak,Schwinden, Mark D.,Zheng, Bin,Kissick, Thomas P.,Patel, Bharat,Humora, Michael J.,Quiroz, Fernando,Dong, Lin,Hsieh, Dau-Ming,Heikes, James E.,Pudipeddi, Madhusudhan,Lindrud, Mark D.,Srivastava, Sushil K.,Kronenthal, David R.,Mueller, Richard H.
-
p. 323 - 328
(2013/09/06)
-
