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) e ee oe ococ: CH2het coea c ocu- C=C pya;

) e e a eee ococ: 2, 3, 5 a. nupuu. B cox cpyypx coeax ooe pa e e;

- pae, oaae opaeoe e a epy aoc cae c oee ococ: CH2het coeax c ocu C=O pya cu-mpuauuo, a ae CH3 pya coeax c NH, N, C=O, CH, C=C;

3) pae, oope epe e oeee o ooe epo aoc. Cpe x pa:

a) xapaepe aoocx coee: SO2 pya coeax c N C=C pya; py NH2 N coeax c SO2, C=C C=O pya; ocupynna coeax c paea N=C CH2het;

) pae, xapaepe yepeoocx coee: 1, 2, 4 - Ar pax coeax c C=O NO2 pya; coea C c C=O, C=N; ocupynna coea c N=C 1, 4-Ar; pae N=C pcyc aoo N, C CH3 py; coea CH2het c C=C, CH2 N=C paea; CH3 pya coeax c C=O, C=C, N=C;

N coea c CH2het C=O pyo; ucopo pcyc py NO2 1, 2, 4-Ar.

Ta opao, e cpyypx pao a poee epo aoc ococ, oeeoe paax papaoax oee pooa, ec ooce aeo cee oycoeo xapaepo aoo opye paeo oeyax. Te e eee, e aoee ycoe xapaepe pa aoc ococ, oope oy eo cooac p pooe ae ox epo-ax coee.

4. Papaoa aa aeaecx oee pacoaa pooa oppeoc pacex pee, oyex peyae cceoa, epy oepe, opeeec a ocoe ocoepoc aeaecx oee pacoaa pooa ax eax coee.

p x oppoa appoac pae xapaepc, ae a oe coca oyax opo, pcece opo oopa pao peae aop.

B aece paox a cooa p oe, oope xapaepyc aoee co ypoe ocoepoc, a. 1.

Taa 1 - Heoope xapaepc aeaecx oee pooa Moe (c- ocoepoc1 peyao co coee c ocoo- co po coee- pooa o aopa I IIoaa paeo, ao oye- oa, /a (ceo acca /ax a oe : oee, /eax), % (PH) A, B) >C=N- >N-C(O)- I II A 28(nd1) 31(co1) <100 /a M20 90/88/91 92/90/(144) B 40(op1) 45 op1 >5 /a M2 A - 41(sula), 22 (sla) <100 /a 14 87/88/86 89/91/(93) - 30 (sulb) >5 /a M3 A 28(nd1) - <100 /a 15 92/92/92 92/87/(68) B 40(nd2) - >5 /a pueau: 1 - ocmoepocm onpeeemc peymamau coomemcmu ey npooupyeu u cnepuemau au, %; - I- aopum eoempu, II aopum "oocoaue".

Maeaeca oe M1, coppoaa a ocoe oeeoo, cpyypo paopooo pa coee, ae 20 pao peaeo aopa (PH), a. 2.

Taa 2 - Maeaeca oe M1 (PH) pacoaa epo aoc Hoep cy- Oea opaCycpyype ecpop, xoe PH cpyyp oc 1 (-O-) /\* (-N=C) /\ (>C=C<) 0,2 (c-pa) \/** (2,4,6-a. p) \/ (-F) 0,3 (-N=C)-(-N=C)-(-O-) \/ (c-pa) \/ (-F) 0,4 (-N=C)#***( 1,2,4,5-Ar)#( 1,2,3,4-a.p) 0,5 (-CH3) # (1,2,4,5-Ar) # (1,2- Ar) 0,6 (c- pa) # (-F) # (-Na) 0,7 (>C=O) # (1,2,3- Ar) # (-F) 0,8 (-O-)-(>C=C<) \/ (1,2,4-Ar) \/ (-F) 0,9 (-S-) \/ (1,2,4-Ar) \/ (1,3 Ar) -0.10 (1,2,4- Ar) # (1,3 Ar) # (-NO2) -0.11 (-NH-) # (1,2,4- Ar) # (>N-) -0.12 (-CH2-) # (H-het)**** # (>N-) -0.13 (1,2,4- Ar) # (H-het) # (>N-) -0.14 (-C#C-) # (H-het) # (>N-) -0.15 (1,3 Ar) # (2,5- a. aao) # (Ph) -0.16 (-NH-)-(>C=C<) \/ (2,5- a. aao) \/(Ph) -0.17 (-CH3) - (>C=C<) - (>SO2) -0.18 (-NH-)-(>C=C<) -0.19 (-(CH2)2-) # (H-het) # (>N-) 0.20 (2,5-a.aao)\/(Ph)\/(2-a. eoao) -0.pueau: /\* - a oueco ameamueco onepauu ou (u); \/** - a oueco ameamueco onepauu uu (uu); #***- a oueco ameamueco onepauu cmpoa uu (uu, o e u); H-het **** - amo oopoa npu emepoamoe.

Apoa cex oee poeea pepo a 300 coeex. caoeo, o oe ocoep xapaepyc co ypo pacoaa aepax py epo aoc: 86-92 %, a. 1. ooeo ocoepoc oe oe M1 oepea a aeaoo ope, cocoe 15 coee, oopx ec ae o aoc. ocoepoc peyao aea - ooo 70 %.

Ta opao, coppoae aeaece oe oaa xopoe peya pacoaa epo aoc cceoax coee oy cooa pooa aa.

5. Opeeee apae aa eeapaeoo cea oeao ax coee Ha ocoa ax, oyex p oppoa oee, opeee apae cea, cocpypoa oee a ypoe pooa oe oeao- ae coee.

Oco poeypa, peaye p ocpypoa, c:

- op aox coee oa, ocoa a aae cpyypoo cxoca cceyex coee c pac aoa aoc;

- opeeee x eeo cpoe, aoee aopx ae c o pe aoc;

- opeeee aoaeex paeo.

Aa cpyypoo cxoca. opa aox coee, coyex aa, ae oecee pep x cpyypoo cxoca c pacca oeec aoa aoc. pep ocoa a ce pacco cex cceyex coee o x aoo pocpace pao peaeo aopa eoo epe. Haoee epce c cpyyp, acao pee aoy acca ax oopeeo yaee o aoa eax. Bce cceyee coee papoa o ooe oy aoy. ae cooa opeee apae oa.

Haoee epcee oa cpyyp oy oee ecoo o: a) pooe cyooe, y oopx coca aecee p poo paoo ax xo oc-pya, oa e eocOCH / ee py ece N SO NH CO NH N apoaec apo c aeceN S CH CH py COOCH3 p., apep, (I) cpyypa (I) - pa aoc 1.

CH3 CHH3C O N C CO O O CH) eepoece pooe eN O oo co, oope coepa ao N O CHcopoa, ca e e(II) ce cce, apep, coeee (II) CH pa 1. N CH N SO NH CO NH N ) cpyyp, coepae oeaN O CH oe ece cce aocoep(III) ae eepo, apep, cpyypa CH S CH CH N (III) pa 2.

SO NH CO N N N cpyyp cpex x pao Cl NH CH CH oa ac coep o e(IV) Cl O CHcoo aoo Cl cocae aecee apoaecx o pcoee- Cl O NOx eocpeceo y, apep, (V) coee (IV) (V).

Aa apae oa cceyex coee. Hapae oa cceyex coee, . e. op aeex paeo ocyec a ocoe oeo, paccax eoa eop p, c yeo ypoeypoo aoec. Oocoae opa aaec o, o aee, epy oepe, peaaec pae, oop ae p cao aopo opye, oc a a aoc.

Oe eee oa cceoax coee c ae:

aoa oopoa, axoeoc p eepoaoe (apep, p aopye, cao c pyo SO2, a coee a A, pc. 3); aoa Cl (apep, a A, pc. 3); eepoa aoa oopoa pocpy (a B, pc.3); oa ecx cce: 1, 2- Ar, 1, 2, 3- Ar, 1, 4- Ar aea aecee poo e (Cl, SH OH), pc.3.

XXN Y N O N N SO2 NH CO NH Z X H Cl N A CO OH B MM20 MT -H-het -het -S- - CF3 -NH- -Na- -Cl >CH- >N- >CH2 >C=C< paea Pc. 3. Aece pae, epy oepe peaaee ae pueaue: no ocu Y yaaa o ucceyex coeueu, omopx npeaamc aee npueee no ocu X paem.

Ba oeo ec oooc yea a ocepeao ca pa pyx ooecx coc, apep, ocpo ococ 50. ooy ae opeee apae oa, cae c xapaepca ococ. p oa, opepoao a y ococ, aoee peoe ae ceye pae: Cl o-ooe o-ae e, pope aece, ao copoa OCH3-py o- - ooex p apoaeco apoe, ae ; coea C=C py pooo a Cl.

Ta opao, oo oe, o oe ee apae oa oye ax eocx coee coaa.

6. Moeyp a oeao-epcex coee Heoxooc oec epa a oe ee cce pace p opaoao ocpypoa oe epe opaaec eoxooc pacpe oo cpyype oeax oapaoopo (ax cycpyyp). apaoop oy e a peeax ooo cceyeoo acca, a ecox acco.

B cooec c ocpypoae ox epcex coee ocyeceo a ocoe ooo ecox acco coee a o oo y (epa aoc), a o oecy coc (epa aoc ocy, % oc). p ae o eco ooec y coacyc pee o opy aox cpyyp, aee o paea.

B ao x apae cooa coee, ee acay epy cxoca c pace aoa aoc, oop pee ceye poeyp aa: aa oa c aeo ooo paea o eco paea, cxea 1; oopeea aea ecox paeo, cxe 2, 3.

B eoo pe 2-[(4,6- eocp-2-) oc] -6- (eoco ) eoo co (cpyypa II, cxea 1), aop apaee cea a o epo aoc, a o ococ ec aea apoaecoo apoa (pae 1 oac aopo ae a pc. 4).

Pc. 4. Opeeee apae oa coee II o epo aoc (A) ococ (T) Boo ae ae pyx paeo, oooec o pacooex y, a eo: CO, CH3-py, pc 4. Heeae e ae a o aoc, a o ococ, c pae, pacooee oac eeaeo ae (pc. 4), apep, ee eepoa, ao copoa.

aoa cpyypa II 3.

H COOC OCH CHCH3 COOCHN N 15. 16. 13.

N OCHC N O CH3 N HN CO O H3CO N C 6.

N O N N 4. 10.

9.

N 1. N OCHOCH CO O CH3 H CO N C 2.

5.

CH 17. 12. 14.

O N O CH18.

(VI) 7.

(VII) 8.

20. 11.

CH CH N O CH19.

H C C N OCH H CO N C CH OCH OCH N N CH H COOC O H COOC O H CO N C N N COOCH OCH OCH OCH N Z (IX) (VIII) O N OCH CHCHe Z= -O- (XII), H3CO CO N C N OCHH3CO CO N C C N OCH>CO - (XIII), >N- O N OCHO N OCH(XIV) N OCHN OCH(X) (XI) Cxea 1. Cpyyp, ceeppoae aeo ooo paea - apoaecoo apoa, oeeoo eo (1-oe eco) o coca eo eea (C~C py 2-oe eco).

pueaue: upo c moo ooae nopo (oepeocm) ae; npoyouo ee aeee u oue paem, uopamuocm ux npueea maue 4.

Taa 4 - pae, cooae p ocpypoa, x a aoc pae x opaoc T 1* T 2* T 3* 1. -CH3 0,276 2. (-CH3)-(-O-) 0,475 3. (-CH3)-(-N=C<)(-O-) 0,4. >N- 0,134 5. (>N-)-(-N=C<) 0,180 6. (-O-)(>N-)-(>CO) 0,7. -NH- -0.208 8. (-NH-)-(>CO) 0,028 9. (-NH-)-(>C=C<)-(-F) 0,10. >CO 0,264 11. (>CO)-(>C=C<) 0,201 12. (>CO)(-NH-)-2,4,6-pa 0,13. >SO2 -0,046 14. (>SO2) - 1,2,3-Ar 0,138 15. (>CO)-(>C=C<)-(>SO2) 0,16. -N=C< 0,399 17. (-N=C<)(-O-) 0,534 18. (-N=C<)-(>C=C<)(>CO) 0,19. -O- 0,781 20. (-O-) - 2,4,6-p 0,454 21. (-N=C<)(-O-)-(-N=C<) 0,22. -S- -0,160 23. (-CH3)-(-S-) -0,100 24. (-S-)-(>C=C<)-(>C=C<) -0,25. -F 0,290 26. 1,2,3-Ar(-F) 0,100 27. (-F)(>C<)-(-F) 0,28. >C=C< 0,141 29. (>C=C<)-(-F) 0,209 30. (>CO)-(>C=C<)-(>C=C<) 0,31. 1,2,3-Ar 0,033 32. (-O-) - 1,2,3-Ar 0,038 33. (-F) - 1,2,3-Ar (-F) 0,34. 1,4-Ar -0,016 35. (>SO2) - 1,4-Ar 0,022 36. (-NH-)-(>SO2)-1,4-Ar 0,37. 1,2,4,5-Ar 0,203 38. 1,2,4,5-Ar (-F) 0,203 39. (-N=C<)-1,2,4,5-Ar-(-O-) 0,40. pa 0,308 41. (-O-)-c-pa 0,308 42. c-pa(-NH-)-(>CO)0,43. 2,3,5-p 44. (-O-)- 2,3,5-p 0,175 45. (-N=C<)-2,3,5-p-(-O-) 0,0,46. 1,4,5-pao 47. (-N=C<)-1,4,5-pao; (-O-)48. (-N=C<)-1,4,5-pao-(-O-) 0,0,175 1,4,5-pao 0,pueaue: *- 1- ucxoe paem, 2- paem ooo opyeu, 3- paem mpooo opyeu.

Ha cxeax 2, 3 pee cpyyp, oyee aeo ecox paeo, ex pay oepeoc, a o oo (cxea 2), a o eco y (cxea 3).

11. C H 2.

4. C H 3 N N 10. 19.

N 7.

8. 6.

S O N H C O N H N 5. 12. 16. 15. 1, 8. 9C H.

2 1. 14.

N S O N H C O N H N N 3. 13.

19.

19.

N 4. 10. O C H 6. 18. 17.

O C H 1, (XV) aoa cpyypa III C H N N C H N S O N C O N H N N O C H O C H (XVI) Cxea 2. Cpyyp, ceeppoae oopeeo aeo yx paeo:

o apae 1,2 poeea aea 1-o eca (apa-ea) oopeeo 2-oo eca - (aapoeapea);

o apae 1,3 - 1-o eca (apa-ea) oopeeo 3-o eca (oopoa aopy).

pueaue: upo c moo, a u a cxee 1, ooae nopo (oepeocm) ae;

npoyouo ee aeee u oue paem. Coeueue XVI cumeupoao (cume ocyecme ucmumyme HTȻ AH P B.T. uxaoo).

Moa, pee a o cxee, p oo aa oa, .. eoope cycpyyp, cocae pae, e ocaoo co a aoc (aopya, coepaa ao oopoa 12 eco; ee aapoeapea 4, 8-10 eca).

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