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Letitia Biweeklyreport 2

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 ,-.$/$  -5= '()01&  39 +0* 72+34,5,5H/*7*:+3/ 73;:8*M% N2 ;3=,92,5@ +0* =,99*/*5+ :36,+,356 35 +0* 72+34,5,5> D* 6+/,<* +3 @*+ 6*8*7+,<* E,5=,5@ +3 +0* @*5*+,7-882 ;3=,9,*= /*7*:+3/6 3<*/ +0* 5-+?/-8 /*7*:+3/6 A6** 9,@?/* #NB% G0,6 :/3J*7+ ,6 ,5 7388-E3/-+,35 D,+0 +0* G3/,, @/3?:% O,@?/* #% L% 12+34,5,5 -+ ,+6 /*7*:+3/P6 E,5=,5@ :374*+> N% Q<*/<,*D 39 /*6*-/70 7357*:+ NN NHNHN OHTyr318Asp262Tyr250Val248HH1 234  27,&8'+59 :+,/6 234 ..)6 78 964 ):- 983 -(;983-<- 6= 9) ;->?3 9<; !(%&;& <=  R*D -::/3-70 +3D-/=6 +0* 625+0*6,6 39 9) ;- HS*-+,5 T*9*/*57*U 13/=*/> L% )%> .?E*=,> N% V%> S0-5@> .%> W-/4> L% X%> O366> O% Y%> Z V,*/7*> N% .% A! #'B% V*/3M,=*H60?5+ 6?E6+/-+*H6:*7,9,7,+2 93/ +0* .-8;35*88- +2:0,;?/,?; Q !H=*:*5=*5+ +TRL ;3=,92,5@ ;3533M2@*5-6* AX,-[B% @<6783A<-9)(  > *$ A'\B> \#]!^\#_\ 2*5,,&#$ :+,/6   G3+-8 625+0*6,6 39 9) ;- HS*-+,5 G/-56HS*-+,5 D-6 ;-5-@*= +3 E* 625+0*6,F*=% G0* 625+0*+,7 /3?+* 6+-/+*= D,+0 625+0*6,6 39 -873038 > +0/3?@0 N37 ! Q -5= -;,53 -873038 /*-7+,35 -5= 93883D*= E2 .D*/5 3M,=-+,35% L9+*/ :*/93/;,5@ .D*/5 3M,=-+,35 -5= `Y[ 38*9,5-+,35> ? D-6 :?/,9,*= ?6,5@ 738?;5 70/3;-+3@/-:02% )-+*/> +0* *6+*/ D-6 /*=?7*= ?6,5@ WINL) +3 ,+6 73//*6:35=,5@ -873038 -5= +0*5 -7,= =*:/3+*7+,35 39 RHN37 @/3?: D-6 =35*% G0* 9,5-8 6+*: D-6 . @  -/28-+,35 39 A -5=  B +3 3E+-,5 9) ;- HS*-+,5 A C B% G/-56HS*-+,5 D-6 :?/,9,*= E2 VG)1 -5= 9/**F*H=/2,5@ 93/ WX.QHD-+*/ /*;3<-8% H 2 NOHOOHNHO 12 88%Et 3 N (1.50 eq)CH 2 Cl 2 , 0 °C to rtBoc 2 O (1.0 eq)1. DIBAL (2.8 eq), CH 2 Cl 2 2. 2 M HCl, 2 hHClãH 2 NOHNNNHNClNNNHNHNOH 5 (1.2 eq) 67 K 2 CO 3 (2.5 eq) n  BuOH110 ° C, 5 h 5 DBU (1.2 eq)LiCl (2.5 eq)OHNOOOEt(EtO) 2 POOEtOCH 3 CN rt, 5 h(3.0 eq) 4 OONHOCH 2 Cl 2 , -78 ° C to rtDMSO (4.0 eq)oxalyl chloride (2.0 eq) 4.0 eq Et 3 N (5.0 eq) 3   G0* 6-;:8* 39 +/-56HS*-+,5 A+SB D-6 0-5=*= +3 V/39% C70,=- 93/ 9?/+0*/ +*6+,5@ 35 +/-56@*5,7  ,) B<:6.-<-  7-//2,5@ aOV /*:3/+*/> D0,70 ,6 735+/388*= E2 'CD  625+0*+,7 :/3;3+*/ A 'CDEEFGH B% G0* 9,@?/* E*83D 603D*= *M:/*66,35 39 G1.UUaOV ,5 6033+ ;*/,6+*; ?:35 ,5+/3=?7+,35 39 +S D0,70 7359,/;*= +0* -7+,<,+2 39 625+0*6,F*= +S% O,@?/* ! W36* /*6:356*6 39 G1.UUaOV E2 %# bX -5= # bX 9) ;- HS*-+,5 H 2 NOHOOHNHO 12 88% (LS-28)Et 3 N (1.50 eq)CH 2 Cl 2 , 0 °C to rtBoc 2 O (1.0 eq)1. DIBAL (2.8 eq), CH 2 Cl 2 2. 2 M HCl, 2 hHClãH 2 NOHNNNHNClNNNHNHNOH 5 (1.2 eq) 67 K 2 CO 3 (2.5 eq) n  BuOH110 ° C, 5 h 5 DBU (1.2 eq)LiCl (2.5 eq)OHNOOOEt(EtO) 2 POOEtOCH 3 CN rt, 5 h(3.0 eq) 4 OONHOCH 2 Cl 2 , -78 ° C to rtDMSO (4.0 eq)oxalyl chloride (2.0 eq) 4.0 eq Et 3 N (5.0 eq) 3 19% (over 2 steps, LS-34)56% (LS-35)69% (LS-36)  .25+0*6*6 39 72+34,5,5 =*/,<-+,<*6 .70*;* ' .25+0*6,6 /3?+* +3D-/= 72+34,5,5 =*/,<-+,<*6 T*-@*5+6 -5= 735=,+,356U A-B !> \H=,7083/3:?/,5*> c ! 1Q ' > ; N?Q`> ## d1> K 0e AEB   \H1083/3H!H98?3/3:?/,5*> c ! 1Q ' > ; N?Q`> ## d1> K 0e A,B :0*528E3/35,7 -7,=> :-88-=,?;AIIB -7*+-+*> +*+/-E?+28-;;35,?; E/3;,=* A,,,B> A<B :2//38,=,5* A5*-+B> ] d1> +,;* +3 E* =*+*/;,5*=e A,<B> A<,,B :,:*/,=,5* A5*-+B> ] d1> +,;* +3 E* =*+*/;,5*=e A<,,,B -5,8,5* A5*-+B> ] d1> +,;* +3 E* =*+*/;,5*=
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