H2020Индивидуална стипендия2020–2022

AsymmFlow · Go with the continuous flow: Asymmetric Synthesis of Bioactive Alkaloids by Multistep Continuous-Flow Processes

„Хоризонт 2020“ — Действия „Мария Склодовска-Кюри“

Период
2020-09-01 → 2022-08-31
Финансиране от ЕС
160 932 €
Участници
1
Схема
MSCA-IF

Линиите свързват координатора с партньорите.

Накратко на български

Нови катализатори се тестват за по-бързо и екологично създаване на специфични молекули, като производните на тетрахидро-бета-карболина. Тези съединения имат противораково и противомаларийно действие, което може да намали разходите и времето за производство на лекарства.

Този кратък обзор е генериран от изкуствен интелект

Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.

Резултати накратко

Go with the continuous flow: Asymmetric Synthesis of Bioactive Alkaloids by Multistep Continuous-Flow Processes

In the Realm of Chemistry, asymmetric synthesis has a prime importance as it allows creation of optically pure chemical entities. The synthesis of preferred enantiomer is highly desirable when seeking for specific biological activities owing to the importance of chirality. AsymmFlow delineates synthesis, characterization and application of novel asymmetric supported organocatalysts for enantioselective Pictet-Splengler cyclization in continuous flow/batch to produce tetrahydro-β-carboline (THβC) derivatives. The proposed immobilization strategy gives access to synthesize reusable, robust and stable catalytic systems for asymmetric continuous-flow processes. The overall aim of AsymmFlow is to provide new sustainable tools for the synthesis of tetrahydro-β-carboline (THβC) derivatives, ranging from quaternary substituted and spiro compounds, which show potent anticancer and antimalarial activity. The advances provided through the project could be translated in future reduced cost and time production of such drugs. Thus, the results of the current project could be translated to an economic impact on human health. Furthermore, the explored synthetic route involves continuous flow chemistry and is in alignment with the principles of green chemistry; thus, the project also contributes with a positive impact on the environment. AsymmFlow proposes the use of reusable immobilized organocatalysts by integrating them into continuous flow reactors to establish faster, safer, and a greener protocol for the enantioselective synthesis of THβC derivatives. The specific objectives of the action have been: 1. Synthesis and characterization of asymmetric immobilized catalysts starting from proline and BINOL derivatives 2. Optimization of reaction conditions for the asymmetric synthesis of THβCs and Michael adducts under batch/continuous flow operation using immobilized catalysts 3. Synthesis of quaternary tryptolines, such as Spiroindolinones, and indoloquinolizidines in continuous flow.

Текст от CORDIS, на английски · Данни: CORDIS, © Европейски съюз

Цел на проекта

In the Realm of Chemistry, asymmetric synthesis has a prime importance as it allows creation of optically pure chemical entities. The synthesis of preferred enantiomer is highly desirable when seeking for specific biological activities owing to the importance of chirality. AsymmFlow delineates synthesis, characterization and application of novel asymmetric supported organocatalysts for enantioselective Pictet-Splengler cyclization in continuous flow/batch to produce tetrahydro-β-carboline (THβC) derivatives. The proposed immobilization strategy gives access to synthesize reusable, robust and stable catalytic systems for asymmetric continuous-flow processes. We aim to develop a sustainable and selective protocol which would give easy access to bioactive substituted-THβC moieties and thus fulfils the demand aiming at lowering their prices in global markets. In particular, the synthesis of the drug Tadalafil usually suffers for poor enantioselectivity, prolonged reaction times, and scale-up issues. It is expected that the development of an alternative protocol for the synthesis of Taladafil will solve those common synthetic challenges and thus, will be highly useful to bring down the market price of this drug all over the world.

Оригинален текст от CORDIS (на английски).

Участници

  • FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA · TARRAGONAКоординаторИспания

Връзки

Данни: CORDIS, © Европейски съюз