A continuous process for making N,N-dimethylacrylamide (NNDMA) is disclosed which uses a commodity chemical, namely vinyl chloride (VCl), which is amidated with dimethylamine (DMA) and carbon monoxide in the presence of a supported palladium(O) triorganophosphine catalyst used under conditions where the ratio of P/Pd is critical. The continous process unexpectedly provides the catalyst with long life because the reaction can be carried out in a moving bed of catalyst in the presence of enough acetonitrile solvent to prevent deposition of DMA.HCl, formed during the reaction, in the pores of the catalyst support.
BACKGROUND OF THE INVENTION
Cross Reference to Related Application
This application is a continuation-in-part application of Ser. No. 161,710 filed Feb. 29, 1988 now U.S. Pat. No. 5,159,113 which, in turn, is a continuation-in-part application of Ser. No. 683,840 filed Dec. 19, 1984, now abandoned.
Novel phosphine and phosphine oxide ligands are prepared using polymeric supports. These compounds can be easily cleaved from the support, and along with the corresponding supported compounds, used as ligands in the preparation of novel, metal-complexed catalysts. The ligands are obtained by combinatorial synthesis. A process for preparing coumarin by contacting salicylaldehyde with an acrylate is also provided.
Novel phosphine and phosphine oxide ligands are prepared using polymeric supports. These compounds can be easily cleaved from the support, and along with the corresponding supported compounds, used as ligands in the preparation of novel, metal-complexed catalysts.
The invention relates to novel 17.beta.-substituted 4-azaandrostane derivatives of general formula (I), ##STR1## wherein R means hydrogen or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.2 are the same or different and stand for hydrogen or a C.sub.1-4 alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; or R.sup.1 and R.sup.2 together means an .alpha.,.omega.-alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and --- bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general formula (I). The compounds of general formula (I) exert a 5.alpha.-reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseases, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.
