1335210-35-9

Usage

Uses

Used in Pharmaceutical Industry:
(4R,12aS)-N-(2,4-Difluorobenzyl)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxaMide is used as an intermediate in the preparation of Dolutegravir, an integrase inhibitor for HIV-1 infection therapy. It plays a crucial role in the synthesis of Dolutegravir, which helps in the treatment of HIV-1 infection by inhibiting the integrase enzyme, thereby preventing the integration of the viral DNA into the host cell's genome.

Upstream product

• 127958-23-0 methyl 2-[(dimethylamino)methylene]-4-methoxy-3-oxobutanoate 
• 1335210-26-8 methyl 2-(((2,2-dimethoxyethyl)amino)methylene)-4-methoxy-3-oxobutanoate 
• 1335210-34-8 (4R,12aS)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8, 12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid 
• 72235-52-0 2,4-Difluoro-benzylamine 
• 41051-15-4 4-methoxyacetoacetic acid methylester 
• 61477-40-5 (R)-3-amino-1-butanol 
• 1335210-23-5 1-[2,2-bis(methyloxy)ethyl]-5-(methyloxy)-6-[(methyloxy)carbonyl]-4-oxo-1,4-dihydro-3-pyridinecarboxylic acid 
• 1550-35-2 2,4-difluorobenzaldehyde 

Downstream Products

• 1051375-19-9 (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2′:4,5]pyrazino-[2,1-b][1,3]oxazine-9-carboxamide sodium salt 
• 1051375-16-6 dolutegravir 

Relevant academic research and scientific papers

Dolutegravir key intermediate solvate polymorph as well as preparation method and application thereof

The invention discloses a dolutegravir key intermediate solvate polymorph as well as a preparation method and application thereof. An X-ray powder diffraction (XRPD) pattern of the polymorph has characteristic peaks at the following angles of 2 theta +/-0.2 degrees: 6.93, 7.84, 8.42, 9.58, 11.14+/-0.2, 12.00, 13.15, 15.04, 15.31, 15.67, 16.20, 16.95, 17.54, 19.18, 19.97, 21.29, 21.82, 22.36, 23.55, 26.00 and 28.47, wherein n ranges from 0.2 to 1.

CONTINUES FLOW PROCESS FOR THE PREPARATION OF ACTIVE PHARMACEUTICAL INGREDIENTS - POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVES AND INTERMEDIATES THEREOF

The present invention discloses continues flow process for the preparation of polycyclic carbamoyl pyridone derivatives and intermediates thereof. In particular, the present invention discloses a process for the preparation of intermediate. Formule (V).

A kind of improved lu tewei preparation process (by machine translation)

The present invention provides anti-aids drugs lu tewei improved preparation process, and for lu tewei bulk drug process control study of the diastereoisomeric synthetic intermediates 6' and its preparation method. The process for preparing the simple routes, simplified for intermediate purification processing, in addition this invention obtained the diastereoisomeric synthetic intermediates 6' help for lu tewei raw material preparation process of quality research. (by machine translation)

7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

Dolutegravir (DTG), an important active pharmaceutical ingredient (API) used in combination therapy for the treatment of HIV, has been synthesized in continuous flow. By adapting the reported GlaxoSmithKline process chemistry batch route for Cabotegravir, DTG was produced in 4.5 h in sequential flow operations from commercially available materials. Key features of the synthesis include rapid manufacturing time for pyridone formation, one-step direct amidation of a functionalized pyridone, and telescoping of multiple steps to avoid isolation of intermediates and enable for greater throughput.

A new method for preparing lu Tewei (by machine translation)

A process for preparing lu Tewei (E) new method, relates to the field of pharmaceutical chemistry, comprising the following steps: step 1) by the compound (A) with 2, 4 - two fluorine animal pen amine condensation reaction to obtain compound (B) steps 2) compound (B) removing the aldehyde protecting group to obtain the compound (C) step 3) compound (C) with R - 3 - amino - 1 - butanol on the ring by the reaction of the compound (D) step 4) compound (D) by the methylation reaction to occur after lu Tewei (E). This invention adopts the new line, and to the continuous optimization of the reaction conditions, so that the overall yield is raised greatly, as the compound (A) as a starting material and calculate the total yield is 75% or more, in a single reaction yield is 90% or more. (by machine translation)

PROCESS FOR THE PREPARATION OF DOLUTEGRAVIR

Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.

PROCESS FOR THE PREPARATION OF DOLUTE-GRAVIR AND INTERMEDIATES THEREOF

The present disclosure relates to processes for the preparation of dolutegravir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of dolutegravir.