Abstract: The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S)-camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily available 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.

Abstract: A process for synthesizing syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof from the corresponding keto-hydroxy compounds, which process comprises: providing a reaction medium comprising sodium borohydride and an alkoxydialkylborane compound; treating the keto-hydroxy compound with said reaction medium under conditions wherein a cyclic boronate ester is formed; and cleaving the cyclic boronate ester to obtain the dihydroxy product.The product compounds, or derivatives thereof, are useful as anti-atherosclerotic agents.

Abstract: Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.

Abstract: An improved process for preparing certain nitrogen-containing mono- and bicyclic ACE inhibitors comprising reacting an .alpha.-alkyl amino acid with a disulfide compound to form a thioester intermediate, which intermediate is then amidated with a mono- or bicyclic amino acid. The invention also relates to the novel thioester intermediates prepared by the first step of the process.