Bioactive Benzisothiazole Morpholine Ketone Derivatives (ii)

ABSTRACTSevent.ee[1 N'--[subst i tuted pyr imi (1 i [1 (l,:1, 5--tr i;[z i l1t') 2. y l I -a---chI oroacety l ureas (5a' 5q) were sy11t l1(3s i zcd f'rom C I (:lIi:.(:()I)(t,fI, i nt ll ree s t r'[')s. S i x t}(1cn o f' t l1etn a ro now cf)lItr)otfn(Is. lt'1;-lc l. i {)lI f) I.':()lnI)oLln(ls (5f1--5q) and Na sa1 t of sacch;1r i n g i ve s i x t()e11 N- [ N'-(slJl,s 1. i t u l'(ld pyr i m i d i n--2--y l ) --ace ty 1 u ro i do] -' l, 2--b()nz i s() t.I1 f flz() -l i nt)--:1--ox() l, 1 --d iox i de dor ivat i ves (6a--6l1) an(J N-- [N'' (4 --ln(i I.l1()xy l--6-- lnethy 1 -- l, 3, 5-- tr iaz ine--2--y l ) --ace ty 1 ure ido] -- l, 2--henz i soth ia-zt1 i ne--3--ox()--l, l--dioxi de derivat i ve (6q). A l ] of th(}m;1re newc()mpoun'ls. The s truc ture of the compounds (5) fln(l (6) wtIrec()n l' i rmed hy IR, 'HNMR, MS and e l eln()n ta1;1l1;l 1 ys i s.S(' r i (}s (5)' N-- (subst i Lute(J nyr im i (J i n--2 y l ) --(x -~cl1 l or()II(t() l y l 1lt'(I;l!;S()r i es (6): N-- [N'-- (subs t i tu ted pyr imi d i n--2--y:[ ) --ace ty 1 u l-e i d()J -l, 2--benz i s()th iazo l i ne--3--oxo-- .I, l --d i ox i de(()a--6D)C()lnnoun(I ((i(l): N-- [N'x-- (4---nlethoxy l --6--mc t'fly l --' I,:3, 5--. t1. i;1z i lI(. 2 }, l );t(:o t.y l [l r(, i (J()1 --- l, 2.--I1(1nz i so th i a---z(l i rlo--*1' ()x() -' l l l -'(J i ()x i tI('The preliminary biological activities of compounds (5a-Sq) and (6a?q) have been determined. It. I s found that. cninpouiiids with 4梙ydroxypyrimidine (5), such as (Sc), (Sd), (be),(St), (fig) (IC.Show excel lent. inhibitory act. i vi ty for di Co ty I odon p1 ant (such as rape) and these with 憀梒hioropyr i m i (Ii no show obvious promo I or action for plant growth. 1 t also show that some of couripouiids (6) havc a good regulating activity for dicotyledon plant (such as rape) and are safe for monocotyledon plant (such as barnyard grass).