Amines analogues

Tocainide. Tocainide is a po active primary amine analogue of lidocaine. It consists of the (3)-(—) and the more active (R)-(+) enantiomers. 

By conventional tests, secondary amine analogues of 4-phenylpiperidine analgesics lack activity (normorphine is equi-potent with morphine by the intra-cisternal route [48]) many secondary bases of the thebaines,(VII), however, are morphine-like analgesics. These findings lend support to the view that the low potencies reported for many nor-analogues of analgesics are due to distribution factors and not to the failure of such derivatives to associate at the receptor. 

Silver(I) complexes with aromatic amines have been less studied than their aliphatic amine analogues, and in general are much less stable (Table 9).49 52... 

We ignore equilibrium of iminium ion with its imine. Imines are ca 2.5-3 pK units less basic than their saturated amine analogues the imines derived from series 6 and 7 should be fully protonated at the acidities in question. See data in References 74b and 85. 

Thus, the synthesis of trehazolin and its analogues required two precursors, the glycosyl isothiocyanate or amine analogues thereof, and trehazolamine or isothicya-nate analogues, respectively. 

The preparation of amine analogues of the product of Step 3, (E)-N-methyl-4-[3-(5-ethoxypyridin)yl]-3-buten-l-amine, (II), and derivatives is described (2). 

Tae-en, the amine analogue of edta, also called penten, originally synthesised and studied by Schwarzenbach et al. (130, 131) is able to form only a single geometric isomer when acting as a sexadentate ligand coordinated to the Co(III) ion. It exists as a pair of enantiomers. Its absolute configuration was determined by Muto et al. (132). The X-ray structure established that the (+>589-[Co(tae-en) complex is... 

It must be noted that the 7-quinolyl derivative has a nitrogen atom at the same relative position as the highly potent 3 -amine analogue of Combretastatin A-4. 

As discussed in Section IV, photolysis is a mild cleavage method that is attractive for combinatorial drug discovery because products can be released into neutral aqueous solution suitable for direct screening. Amine analogues of the hydroxyl resins described earlier have been reported. Thus, (aminomethyl)-6>-nitrobenzyl supports 7n have been reported on which short peptide amides could be synthesized with cleavage occurring upon irradiation at 350 nm in the presence of ammonia [323]. 2-Nitrobenzhydryl (NBHA) supports 7o have also been used for peptide amide assembly using Boc-protected amino acids. The anchor was unaffected by 4 N HCl-dioxane... 

---