Patent classifications
C07C253/30
Methods and compositions for terpenoid tricycloalkane synthesis
In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of terpenoid cores. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising a terpenoid core or scaffold, such as 6/7/5 tricycloalkanes. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to tunably and scalably assemble common terpenoid cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Continuous synthesis method for ethoxymethylenemalononitrile
Provided is a continuous synthesis method for ethoxymethylenemalononitrile. The method includes the following steps: malononitrile, triethyl orthoformate and acetic anhydride are continuously fed into a continuous reaction device to perform a condensation reaction, to obtain the ethoxymethylenemalononitrile, and in the process of the condensation reaction, the generated ethoxymethylenemalononitrile is continuously discharged; herein, the molar ratio of the malononitrile, the triethyl orthoformate and the acetic anhydride is 1:(0.9-6.0):(2.0-6.0). By adopting the continuous reaction device in the present disclosure, since the amount of materials involved in the reaction per unit time is greatly reduced, a high temperature dangerous area is reduced, and a safety risk is greatly reduced. In addition, through the continuous reactor, the raw materials may be transiently heated to the reaction temperature, so that the decomposition of the raw materials caused by the long-time heating process is avoided, and the yield is significantly improved. Moreover, in the reaction process of the present disclosure, there is no need for a second-class toxic solvent such as a toluene.
Continuous synthesis method for ethoxymethylenemalononitrile
Provided is a continuous synthesis method for ethoxymethylenemalononitrile. The method includes the following steps: malononitrile, triethyl orthoformate and acetic anhydride are continuously fed into a continuous reaction device to perform a condensation reaction, to obtain the ethoxymethylenemalononitrile, and in the process of the condensation reaction, the generated ethoxymethylenemalononitrile is continuously discharged; herein, the molar ratio of the malononitrile, the triethyl orthoformate and the acetic anhydride is 1:(0.9-6.0):(2.0-6.0). By adopting the continuous reaction device in the present disclosure, since the amount of materials involved in the reaction per unit time is greatly reduced, a high temperature dangerous area is reduced, and a safety risk is greatly reduced. In addition, through the continuous reactor, the raw materials may be transiently heated to the reaction temperature, so that the decomposition of the raw materials caused by the long-time heating process is avoided, and the yield is significantly improved. Moreover, in the reaction process of the present disclosure, there is no need for a second-class toxic solvent such as a toluene.
PROCESS FOR THE PRODUCTION OF ANTITUMOUR PHARMACEUTICAL COMPOSITIONS USING PUSH-PULL BUTADIENES, COMPOUNDS AND USES THEREOF
The present invention reports the obtaining of carbonyl compounds and derivatives, through syntheses with high yield and purity, providing anti-humoral active principles with selective antiproliferative properties and anti-metastatic activity.
The present invention refers to the development of new polyfunctional push-pull butadienes and their O and C-prenylated, benzoylated and iodide derivatives, with high electronic conjugation in the lateral chain. These compounds exhibit high anti-tumor selectivity, causing cell death by apoptosis, also show anti-metastatic and non-mutagenic properties in the experimental studies performed.
PROCESS FOR THE PRODUCTION OF ANTITUMOUR PHARMACEUTICAL COMPOSITIONS USING PUSH-PULL BUTADIENES, COMPOUNDS AND USES THEREOF
The present invention reports the obtaining of carbonyl compounds and derivatives, through syntheses with high yield and purity, providing anti-humoral active principles with selective antiproliferative properties and anti-metastatic activity.
The present invention refers to the development of new polyfunctional push-pull butadienes and their O and C-prenylated, benzoylated and iodide derivatives, with high electronic conjugation in the lateral chain. These compounds exhibit high anti-tumor selectivity, causing cell death by apoptosis, also show anti-metastatic and non-mutagenic properties in the experimental studies performed.
PROCESS FOR THE PRODUCTION OF ANTITUMOUR PHARMACEUTICAL COMPOSITIONS USING PUSH-PULL BUTADIENES, COMPOUNDS AND USES THEREOF
The present invention reports the obtaining of carbonyl compounds and derivatives, through syntheses with high yield and purity, providing anti-humoral active principles with selective antiproliferative properties and anti-metastatic activity.
The present invention refers to the development of new polyfunctional push-pull butadienes and their O and C-prenylated, benzoylated and iodide derivatives, with high electronic conjugation in the lateral chain. These compounds exhibit high anti-tumor selectivity, causing cell death by apoptosis, also show anti-metastatic and non-mutagenic properties in the experimental studies performed.
A PROCESS FOR THE PREPARATION OF 4-CYANOBENZOYL CHLORIDES
The present invention relates to a process for the preparation of 4-cyanobenzoyl chlorides of formula I through reaction of compounds of formula II with a chlorinating agent.
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A PROCESS FOR THE PREPARATION OF 4-CYANOBENZOYL CHLORIDES
The present invention relates to a process for the preparation of 4-cyanobenzoyl chlorides of formula I through reaction of compounds of formula II with a chlorinating agent.
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A PROCESS FOR THE PREPARATION OF 4-CYANOBENZOYL CHLORIDES
The present invention relates to a process for the preparation of 4-cyanobenzoyl chlorides of formula I through reaction of compounds of formula II with a chlorinating agent.
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Process of preparing 3-fluoro-5(((1R,2aR)-3,3,4,4-tetrafluoro-1,2a-dihydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)-oxy)benzonitrile
Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.