Hexahydropyrrolo[3,4-b]pyrrole derivatives, preparation methods and pharmaceutical uses thereof

A method for preparing a compound according to formula (I), wherein, the method comprises the steps of:

• (a) reacting a compound of formula (1c) with a compound of formula (1d) under a peptide coupling condition to produce a compound of formula (1e),
• (b) deprotecting the compound of formula (1e) under a basic condition to produce a compound of formula (1f),
• (c) converting the compound of formula (1f) to a compound of formula (1g) by a coupling reaction or acylation reaction, and
• (d) deprotecting the compound of formula (1 g) to a compound of formula (Ia) in the presence of an acid;
• wherein,
• X is selected from the group consisting of:
• (1) —C1-C3 alkylidene-;
• (2) —C(O)—;
• (3) —S(O)2—;
• (4) —C(O)O—;
• and
• (5) —C(O)NR1—;
• R is selected from the group consisting of:
• (1) H;
• (2) C1-C6 alkyl, which is unsubstituted or substituted by one to three substituents selected from the following group:
• fluorine, chlorine or hydroxyl;
• (3) C3-C6 cycloalkane, which is unsubstituted or substituted by one to two substituents selected from the following group:
• C1-C3 alkyl, fluorine, chlorine, hydroxyl, cyano, C(O)NH2;
• (4) Phenyl, which is unsubstituted or substituted by one to three substituents selected from the following:
• C1-C3 alkyl, fluorine, chlorine, cyano, S(O)2R2;
• and
• (5) 6-membered heterocycle containing one to two atoms independently selected from N atom, above-mentioned 6-membered heterocycle is unsubstituted or substituted by one to three substituents selected from the followings:
• C1-C3 alkyl, fluorine, chlorine, cyano, S(O)2R2;
• Wherein, R1 is H or C1-C3 alkyl;
• R2 is C1-C3 alkyl.