Pietro Mangiaracina

Recent studies on veratrum alkaloids: a new reaction of sodium triacetoxyborohydride [NaBH(OAc)3]

In the presence of a hydroxyl group juxtaposed for participation, NaBH(OAC)3 reduced even ketones in a stereo and regiospecific manner and in excellent yields.

Synthesis and structure–activity relationships of oxime neurokinin antagonists: discovery of potent arylamides

The structural modification of the benzylic ether region of oxime 1 has resulted in the identification of several novel aryl amides as selective or dual NK(1)/NK(2) antagonists.

Synthesis of a carbocyclic analog of quercetin via a barbier reaction

Abstract A six-step synthetic route to the carbocyclic flavanoid 2 is described. The key step involves a 1,4-addition of a tertiary bromide to a α,β-unsaturated ester by the Barbier reaction.

Synthesis of 7,8-acetylenic analogs of hexahydro leukotriene-E4 with agonist and antagonist activities: convenient stereoselective routes to E- and Z-enynes

Abstract E- and Z-enynes available by stereoselective dehydrations of Co 2 (CO) 6 completed and uncomplexed propargyl alcohols 13 and 5 produced acetylenic LT-E 4 analogs with contractile activity similar to leukotrienes. Their 5-desoxy analogs were found to have antagonist activity against LT-C 4 induced contractions on isolated guinea pig lung parenchyma.

Synthesis of butanoic acid 4,4′-[(4E, 6Z, 9Z-pentadecatrien-2-ynylidene)-bis with leukotriene- like activity: Novel acetylenic acetals and dithioacetals as antagonists of leukotriene-C4

Abstract A selective exchange reaction of the symmetrical acetal 5a with protected cysteine readily provided the hemi-thioacetals 9a and 11a related to leukotriene-E 4 . Use of acetylene-bis-(diethyl acetal) 12 led to a facile synthesis of the title compound 17a. Its corresponding hexahydro analogs displayed marked antagonist activity against LT-C 4 induced contractions on isolated guinea pig lung parenchyma.

Transfer hydrogenolysis: an improved synthesis of (R)-(-)-α-Methyl Histamine

Abstract Ammonium formate in the presence of palladium on carbon in methanol reacted with (S)-(+)4-(2-Amino-3-chloropropyl)-imidazole to give optically pure (R)-(−)-α-methyl histamine at atmospheric pressure.