The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide R.sup.3CONR.sup.1R.sup.2. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(R.sup.3CO.sub.2).sub.3—B—NHR.sup.1R.sup.2]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated.

A method for the manufacture of N,N-dialkyllactamide, whereby at least one of the compounds selected from the series made of alkyl lactate, lactide and polylactic acid is mixed with dialkylamine in order to form a reaction mixture, under conditions whereby aminolysis takes place in the reaction mixture. The method is characterized in that the reaction mixture further includes a Lewis acid. As a result of the method, N,N-dialkyllactamides can be manufactured in high yields and with high optical purity.

A method for the manufacture of N,N-dialkyllactamide, whereby at least one of the compounds selected from the series made of alkyl lactate, lactide and polylactic acid is mixed with dialkylamine in order to form a reaction mixture, under conditions whereby aminolysis takes place in the reaction mixture. The method is characterized in that the reaction mixture further includes a Lewis acid. As a result of the method, N,N-dialkyllactamides can be manufactured in high yields and with high optical purity.

A method for the manufacture of N,N-dialkyllactamide, whereby at least one of the compounds selected from the series made of alkyl lactate, lactide and polylactic acid is mixed with dialkylamine in order to form a reaction mixture, under conditions whereby aminolysis takes place in the reaction mixture. The method is characterized in that the reaction mixture further includes a Lewis acid. As a result of the method, N,N-dialkyllactamides can be manufactured in high yields and with high optical purity.

A method i for forming an epoxidized polymer is provided. The method may include mixing an epoxidized plant oil with a synthetic epoxy resin and crosslinking the epoxidized plant oil and the synthetic epoxy resin using a curing agent. The epoxidized plant oil may be formed via: converting plant oil triglycerides to fatty amide alcohols via aminolysis using primary or secondary amines, converting the fatty amide alcohols to epoxidized fatty amide alcohols, and reacting the epoxidized fatty amide alcohols with vinyl monomers to obtain epoxidized plant oil monomers.

A method i for forming an epoxidized polymer is provided. The method may include mixing an epoxidized plant oil with a synthetic epoxy resin and crosslinking the epoxidized plant oil and the synthetic epoxy resin using a curing agent. The epoxidized plant oil may be formed via: converting plant oil triglycerides to fatty amide alcohols via aminolysis using primary or secondary amines, converting the fatty amide alcohols to epoxidized fatty amide alcohols, and reacting the epoxidized fatty amide alcohols with vinyl monomers to obtain epoxidized plant oil monomers.

A method i for forming an epoxidized polymer is provided. The method may include mixing an epoxidized plant oil with a synthetic epoxy resin and crosslinking the epoxidized plant oil and the synthetic epoxy resin using a curing agent. The epoxidized plant oil may be formed via: converting plant oil triglycerides to fatty amide alcohols via aminolysis using primary or secondary amines, converting the fatty amide alcohols to epoxidized fatty amide alcohols, and reacting the epoxidized fatty amide alcohols with vinyl monomers to obtain epoxidized plant oil monomers.

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

The subject matter of the present invention is the novel molecules of formulae E, E′ and F. These molecules prove to be synthesis intermediates that are very advantageous for the manufacture of derivatives of sphingosine or of ceramides functionalized in position 1, with good yields, in which R.sub.1 and R.sub.2 are fatty chains, R.sub.3 is an alkyl group and R.sub.4 is a protective group for alcohol functions. Another subject of the invention is the use of the intermediates of type F for converting same into intermediates of type G, by means of reduction in the presence of lithium borohydride. The G molecules are precursors that are known to make it possible to obtain sphingolipids or sphingomyelin.